4-Substituted Pyrazoline Compounds, their Preparation and Use as Medicaments

ABSTRACT

The present invention relates to 4-substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.

CROSS-REFERENCE TO RELATED APPLICATIONS

This application claims the benefit of priority of U.S. ProvisionalPatent Application No. 60/705,432, filed Aug. 5, 2005, and EuropeanPatent Application No. 05384029, filed Jul. 15, 2005, each of which ishereby incorporated by reference in its entirety.

FIELD OF THE INVENTION

The present invention relates to 4-substituted pyrazoline compounds,methods for their preparation, medicaments comprising these compounds aswell as their use for the preparation of a medicament for the treatmentof humans and animals.

BACKGROUND OF THE INVENTION

Cannabinoids are compounds, which are derived from the cannabis sativaplant which is commonly known as marijuana. The most active-chemicalcompound of the naturally occurring cannabinoids is tetrahydrocannabinol(THC), particularly Δ⁹-THC.

These naturally occurring cannabinoids as well as their syntheticanalogues promote their physiological effects via binding to specificG-coupled receptors, the so-called cannabinoid-receptors.

At present, two distinct types of receptors that bind both the naturallyoccurring and synthetic cannabinoids have been identified and cloned.These receptors, which are designated CB₁ and CB₂ are involved in avariety of physiological or pathophysiological processes in humans andanimals, e. g. processes related to the central nervous system, immunesystem, cardiovascular system, endocrinous system, respiratory system,the gastrointestinal tract or to reproduction, as described for example,in Hollister, Pharm. Rev. 38, 1986, 1-20; Reny and Singha, Prog. Drug.Res., 36, 71-114, 1991; Consroe and Sandyk, in Marijuana/Cannabinoids,Neurobiology and Neurophysiology, 459, Murphy L. and Barthe A. Eds., CRCPress, 1992.

Therefore, compounds, which have a high binding affinity for thesecannabinoid receptors and which are suitable for modulating thesereceptors are useful in the prevention and/or treatment ofcannabinoid-receptor related disorders.

In particular, the CB₁-receptor is involved in many differentfood-intake related disorders such as bulimia or obesity, includingobesity associated with type II diabetes (non-insulin-dependentdiabetes) and thus, compounds suitable for regulating this receptor maybe used in the prophylaxis and/or treatment of these disorders.

SUMMARY OF THE INVENTION

Thus, it was an object of the present invention to provide novelcompounds for use as active substances in medicaments. In particular,these active substances should be suitable for the modulation ofcannabinoid receptors, more particularly for the modulation ofcannabinoid 1 (CB₁) receptors.

Said object was achieved by providing the 4-substituted pyrazolinecompounds of general formula I given below, their stereoisomers,corresponding salts and corresponding solvates thereof.

It has been found that these compounds have a high affinity forcannabinoid receptors, particularly for the CB₁-receptor, and that theyact as modulators e. g. antagonists, inverse agonists or agonists onthese receptors. They are therefore suitable for the prophylaxis and/ortreatment of various disorders related to the central nervous system,the immune system, the cardiovascular system, the endocrinous system,the respiratory system, the gastrointestinal tract or reproduction inhumans and/or animals, preferably humans including infants, children andgrown-ups.

DETAILED DESCRIPTION OF THE INVENTION

Thus, in one of its aspects the present invention relates to4-substituted pyrazoline compounds of general formula I,

wherein

-   x is O or S;-   R¹ and R², independently of one another, in each case represent an    unsubstituted or at least mono-substituted aryl or heteroaryl    radical, which may be condensed with an unsubstituted or at least    mono-substituted mono- or polycyclic ring system;    -   or a saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical, which may be condensed        with an unsubstituted or at least mono-substituted mono- or        polycyclic ring system and/or may be bridged by at least one        unsubstituted or at least mono-substituted alkylene group;-   R³ an unsubstituted or at least mono-substituted aryl or heteroaryl    radical, which may be condensed with an unsubstituted or at least    mono-substituted mono- or polycyclic ring system;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical, which may be condensed        with an unsubstituted or at least mono-substituted mono- or        polycyclic ring system and/or may be bridged by at least one        unsubstituted or at least mono-substituted alkylene group;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical which together with a        saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical forms a saturated or        unsaturated, unsubstituted or at least mono-substituted,        optionally at least one heteroatom as a ring member containing        spirocyclic residue via a common ring atom;    -   a —O—R⁶ moiety; a —NR⁷R⁸ moiety or a —NR⁹—O—R¹⁰ moiety;-   R⁴ represents F; Cl; Br; I; —CN; —NO₂; —NC; —OH; —NH₂; —SH;    —C(═O)—H; —C(=O)—OH; —C(═O)—OR¹⁷;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted aliphatic radical;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical, which may be condensed        with an unsubstituted or at least mono-substituted mono- or        polycyclic ring system and/or may be bonded via an unsubstituted        or at least mono-substituted alkylene group, alkenylene group or        alkinylene group and/or may be bridged by at least one        unsubstituted or at least mono-substituted alkylene group;    -   an unsubstituted or at least mono-substituted aryl or heteroaryl        radical, which may be condensed with an unsubstituted or at        least mono-substituted mono- or polycyclic ring system and/or        may be bonded via an optionally at least mono-substituted        alkylene group, alkenylene group or alkinylene group;    -   a —O—R¹¹ moiety; a —S—R¹² moiety; a —NH—R¹³ moiety or a —NR¹⁴R¹⁵        moiety;-   R⁵ represents H; F; Cl; Br; I; —CN; —NO₂; —NC; —OH; —NH₂; —SH;    —C(═O)—H; —C(═O)—OR¹⁷;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted aliphatic radical;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical, which may be condensed        with an unsubstituted or at least mono-substituted mono- or        polycyclic ring system and/or may be bonded via an unsubstituted        or at least mono-substituted alkylene group, alkenylene group or        alkinylene group and/or may be bridged by at least one        unsubstituted or at least mono-substituted alkylene group;    -   an unsubstituted or at least mono-substituted aryl or heteroaryl        radical, which may be condensed with an unsubstituted or at        least mono-substituted mono- or polycyclic ring system and/or        may be bonded via an unsubstituted or at least mono-substituted        alkylene group, alkenylene group or alkinylene group;    -   a —O—R¹¹ moiety; a —S—R¹² moiety; a —NH—R¹³ moiety or a —NR¹⁴R¹⁵        moiety;-   or R⁴ and R⁵ together with the bridging carbon atom form a saturated    or unsaturated, unsubstituted or at least mono-substituted,    optionally at least one heteroatom as a ring member containing    cycloaliphatic radical;-   R⁶ represents a hydrogen atom;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted aliphatic radical;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical, which may be condensed        with an unsubstituted or at least mono-substituted mono- or        polycyclic ring system and/or may be bonded via an unsubstituted        or at least mono-substituted alkylene group, alkenylene group or        alkinylene group and/or may be bridged by at least one        unsubstituted or at least mono-substituted alkylene group;    -   an unsubstituted or at least mono-substituted aryl or heteroaryl        radical, which may be condensed with an unsubstituted or at        least mono-substituted mono- or polycyclic ring system and/or        may be bonded via an unsubstituted or at least mono-substituted        alkylene group, alkenylene group or alkinylene group;    -   a —P(═O)(OR¹⁶)₂ moiety; a —C(═O)—OR¹⁷ moiety; a —C(═O)—NH—R¹⁸        moiety or a —C(═O)—R¹⁹ moiety;-   R⁷ and R⁸, independently of one another, in each case represent a    hydrogen atom;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted aliphatic radical;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical, which may be condensed        with an unsubstituted or at least mono-substituted mono- or        polycyclic ring system and/or may be bonded via an unsubstituted        or at least mono-substituted alkylene group, alkenylene group or        alkinylene group and/or may be bridged by at least one        unsubstituted or at least mono-substituted alkylene group;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical which together with a        saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical forms a saturated or        unsaturated, unsubstituted or at least mono-substituted,        optionally at least one heteroatom as a ring member containing        spirocyclic residue via a common ring atom;    -   an unsubstituted or at least mono-substituted aryl or heteroaryl        radical, which may be condensed with an unsubstituted or at        least mono-substituted mono- or polycyclic ring system and/or        may be bonded via an unsubstituted or at least mono-substituted        alkylene group, alkenylene group or alkinylene group;    -   a —P(═O)(OR ¹⁶)₂ moiety; a —C(═O)—OR¹⁷ moiety; a —C(═O)—NH—R¹⁸        moiety; a —C(═O)—R¹⁹ moiety; a —S(═O)₂—R²⁰ moiety; or a —NR²¹R²²        moiety;-   R⁹ represents hydrogen or a saturated or unsaturated, unsubstituted    or at least mono-substituted aliphatic radical,-   R¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²⁰, independently of one another,    in each case represent a saturated or unsaturated, unsubstituted or    at least mono-substituted aliphatic radical;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical, which may be condensed        with an unsubstituted or at least mono-substituted mono or        polycyclic ring system and/or may be bonded via an unsubstituted        or at least mono-substituted alkylene group, alkenylene group or        alkinylene group and/or may be bridged by at least one        unsubstituted or at least mono-substituted alkylene group;    -   or an unsubstituted or at least mono-substituted aryl or        heteroaryl radical, which may be condensed with an unsubstituted        or at least mono-substituted mono- or polycyclic ring system        and/or may be bonded via an unsubstituted or at least        mono-substituted alkylene group, alkenylene group or alkinylene        group;-   R¹⁶, R¹⁷, R¹⁸ and R¹⁹, independently of one another, in each case    represent a saturated or unsaturated, unsubstituted or at least    mono-substituted aliphatic radical;    -   or an unsubstituted or at least mono-substituted aryl or        heteroaryl radical, which may be condensed with an unsubstituted        or at least mono-substituted mono- or polycyclic ring system        and/or may be bonded via an unsubstituted or at least        mono-substituted alkylene group, alkenylene group or alkinylene        group;        and-   R²¹ and R²², independently of one another, in each case represent a    hydrogen atom;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted aliphatic radical;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical, which may be condensed        with an unsubstituted or at least mono-substituted mono- or        polycyclic ring system and/or may be bonded via an unsubstituted        or at least mono-substituted alkylene group, alkenylene group or        alkinylene group;    -   a saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical which together with a        saturated or unsaturated, unsubstituted or at least        mono-substituted, optionally at least one heteroatom as a ring        member containing cycloaliphatic radical forms a saturated or        unsaturated, unsubstituted or at least mono-substituted,        optionally at least one heteroatom as a ring member containing        spirocyclic residue via a common ring atom;    -   or an unsubstituted or at least mono-substituted aryl or        heteroaryl radical, which may be condensed with an unsubstituted        or at least mono-substituted mono- or polycyclic ring system        and/or may be bonded via an unsubstituted or at least        mono-substituted alkylene group, alkenylene group or alkinylene        group;        optionally in form of one of its stereoisomers, preferably        enantiomers or diastereomers, a racemate or in form of a mixture        of at least two of its stereoisomers, preferably enantiomers        and/or diastereomers, in any mixing ratio, or a corresponding        N-oxide thereof, or a physiologically acceptable salt thereof,        or a corresponding solvate thereof. The term stereoisomers        includes tautomers as well.

Preferably one or more of the following compounds are excluded

-   [A] ethyl    4,5-dimorpholino-1-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylate,-   [B] methyl    1-phenyl-4,5-di(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxylate,-   [C]    1-(4-chlorophenyl)-4-(hydroxymethyl)-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid,-   [D] ethyl    5-morpholino-1,4-diphenyl-4,5-dihydro-1H-pyrazole-3-carboxylate,-   [E] ethyl    4-(4-chlorophenyl)-1-(4-fluorophenyl)-5-morpholino-4,5-dihydro-1H-pyrazole-3-carboxylate,-   [F] ethyl    1-(4-fluorophenyl)-5-morpholino-4-p-tolyl-4,5-dihydro-1H-pyrazole-3-carboxylate,-   [G] methyl    4-(hydroxymethyl)-1-(2-(methoxycarbonyl)phenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylate,-   [H]    benzofuran-2-yl(5-(4-hydroxyphenyl)-4-nitro-1-(3-phenyl-1H-pyrazol-5-yl)-4,5-dihydro-1H-pyrazol-3-yl)methanone,-   [I]    (5-(benzo[d][1,3]dioxol-5-yl)-4-nitro-1-(3-phenyl-1H-pyrazol-5-yl)-4,5-dihydro-1H-pyrazol-3-yl)    (benzofuran-2-yl)methanone,-   [J]    3-(benzofuran-2-carbonyl)-5-phenyl-1-(3-phenyl-1H-pyrazol-5-yl)-1H-pyrazole-4,4(5H)-dicarbonitrile,-   [K]    (5-(benzo[d][1,3]dioxol-4-yl)-4-nitro-1-(3-phenyl-1H-pyrazol-5-yl)-4,5dihydro-1H-pyrazol-3-yl)(benzofuran-2-yl)methanone,-   [L] ethyl    1-(3-methoxyphenyl)-5-morpholino-4-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylate,-   [M] ethyl    1-(3-methoxyphenyl)-4-phenyl-5-(piperazin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxylate,    which is optionally bonded to copolystyrol,-   [N]    1-(3-rnethoxyphenyl)-4-phenyl-5-(piperazin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxylic    acid, which is optionally bonded to copolystyrol,-   [O] ethyl    5-(4-oxo-2,3-diphenyl-4,5-dihydro-2H-pyrazolo[4,3-d]pyridazin-7-yl)-1,4-diphenyl-4,5-dihydro-1H-pyrazole-3-carboxylate,    optionally in form of one of their stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of their stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a physiologically acceptable salt thereof, or a    corresponding solvate thereof.

The structure of the excluded compounds A to O is depicted below:

Also preferably compounds of general formula I, wherein R⁶ represents abenzofuranyl radical, are excluded.

If one or more of the residues R¹ to R²² represents or comprises an arylor heteroaryl radical, which may be substituted, unless definedotherwise, preferably said aryl or heteroaryl radical may optionally besubstituted with 1, 2, 3, 4 or 5 substituent(s) independently selectedfrom the group consisting of —C₁₋₆-perfluoralkyl, —C₁₋₆-alkylsubstituted with one or more methoxy and/or ethoxy groups, —C₁₋₆-alkyl,—C₁₋₆-alkyl substituted with one or more hydroxy groups, —C₁₋₆-alkylsubstituted with one or more chlorine atoms, —O—C₁₋₆-alkyl,—O—C₁₋₆-alkyl substituted with one or more methoxy and/or ethoxy groups,—S—C₁₋₆-alkyl, —C(═O)—OH, —C(═O)—O—C₁₋₆-alkyl, —O—C(═O)—C₁₋₆-alkyl, F,Cl, Br, I, —CN, —OCF₃, —O—C₂F₅, —O—C₃F₇, —O—C₄F₉, —SCF₃, —SCF₃, —SCF₂H,—SCFH₂, —OH, —SH, —SO₃H, —NH—C(═O)—C₁₋₆-alkyl,—N(C₁₋₆-alkyl)—C(═O)—C₁₋₆-alkyl, —NO₂, —CHO, —-C(═O)—C₁₋₆-alkyl,—C(═O)-C₁₋₆-perfluoroalkyl, —C(═S)—NH—C₁₋₆-alkyl, —CF₂H, —CFH₂,—C(═O)—NR^(A)R^(B), —C(═O)—NH NR^(C)R^(D), —S(═O)—C₁₋₆-alkyl,—S(═O)₂—C₁₆-alkyl, —S(═O)₂-phenyl, —(C₁₋₅-alkylene)—S—C₁₋₆-alkyl,—(C₁₋₅-alkylene)—S(═O)—C₁₋₆-alkyl, —(C₁₋₅-alkylene)—S(═O)₂—C₁₋₆-alkyl,—NR^(E)R^(F), —(C₁₋₅-alkylene)—NR^(E)R^(F), —S(═O)—NH₂, —S(═O),—NH—C₁₋₆-alkyl, —S(═O)₂—NH-phenyl, —NH—S(═O)₂—C₁₋₆-alkyl, cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, phenyl,thiophenyl, phenoxy and benzyl;

whereby in each case the cyclic moieties cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, phenyl, thiophenyl,phenoxy and benzyl can optionally be substituted with 1, 2, 3, 4 or 5substituent(s) independently selected from the group consisting of F,Cl, Br, I, —OH, —CF₃, —CN, —NO₂, —C₁₋₆-alkyl, —O—C₁₋₆-alkyl, —O—CF₃ and—S—CF₃ and

whereby R^(A), R^(B), R^(E) and R^(F), independently of one another,represent hydrogen or —C₁₋₆-alkyl or R^(A) and R^(B) in each casetogether with the bridging nitrogen atom form a radical selected fromthe group consisting of pyrrolidinyl, imidazolidinyl, piperazinyl,piperidinyl, thiomorpholinyl, morpholinyl, azepanyl and diazepanyl whichmay be at least mono-substituted with one or more identical or differentC₁₆ -alkyl radicals

and whereby R^(C) and R^(D), independently of one another, representhydrogen, —C₁₋₆-alkyl, —C(═O)—O—C₁₋₆-alkyl, C₃₋₈-cycloalkyl,—(C₁₋₅-alkylene)—C₃₋₈-cycloalkyl, —(C₁₋₆-alkylene)—O—C₁₋₆-alkyl or—C₁₋₆-alkyl substituted with one or more hydroxy groups or R^(C) andR^(D) in each case together with the bridging nitrogen atom form aradical selected from the group consisting of pyrrolidinyl,imidazolidinyl, piperazinyl, piperidinyl, thiomorpholinyl, morpholinyl,azepanyl and diazepanyl which may be at least mono-substituted with oneor more substituents independently selected from the group consisting—C₁₋₆-alkyl, —C(═O)—C₁₋₆-alkyl, —C(═O)—O—C₁₋₆-alkyl,—C(═O)—NH—C₁₋₆-alkyl, —C(═S)—NH—C₁₋₆-alkyl, oxo (═O), —C₁₋₆-alkylsubstituted with one or more hydroxy groups,—(C₁₋₆-alkylene)—O—C₁₋₆-alkyl and —C(═O)—NH₂.

More preferably said aryl and heteroaryl radicals may optionally besubstituted with 1, 2, 3, 4 or 5 substituent(s) independently selectedfrom the group consisting of —CF₃, —C₂F₅, —C₃F₇, —C₄F₉, —CH₂Cl, —CHCl₂,—C₂H₄Cl, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl,tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —CH₂—OH, —CH₂—CH₂—OH,—CH₂—CH₂—CH₂—OH, —O—CH₂—O—CH₃, —O—CH₂—CH₂—O—CH₃, —O—CH₂—O—C₂H₅,—C(OCH₃)(C₂H₅)₂, —C(OCH₃)(CH₃)₂, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,—O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,—S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, —C(═O)—OH,—C(═O)—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C₃H₇, —C(═O)—O—C(CH₃)₃,—O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂, —O—C(═O)—CH₂—CH₂—CH₃,—O—C(═O)—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —O—C₂F₅, —O—C₃F₇, —O—C₄F₉,—SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —SO₃H, —NH—C(═O)—CH₃, —NH—C(═O)—C₂H₅,—NH—C(═O)—C(CH₃)3, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃,—C(═O)—CF₃, —C(═O)—C₂F₅, —C(═O)—C₃F₇, —C(═S)—NH—CH₃, —C(═S)—NH—C₂H₅,—CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —C(═O)—NH—NH—CH₃, —C(═O)—NH—NH—C₂H₅,—C(═O)—NH—NH₂, —C(═O)—NH—N(CH₃)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —S(═O)₂-phenyl, —NH₂, —NH—CH₃,—NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —CH₂—N(CH₃)₂, —(CH₂)-morpholinyl,—(CH₂)-piperidinyl, —(CH₂) -piperazinyl, —(CH₂)—N(C₂H₅)₂, —CH₂—N(C₃H₇)₂,—CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅), —S(═O)—NH₂, —S(═O)₂—NH—CH₃,—S(═O)₂—NH-phenyl, —NH—S(═O)₂—CH₃, cyclopropyl, cyclobutyl, cyclopentyl,cyclohexyl, pyrrolidinyl, piperidinyl, phenyl, thiophenyl, phenoxy andbenzyl, whereby said thiophenyl radical can be substituted with 1, 2 or3 substituent(s) independently selected from the group consisting of F,Cl, Br, methyl, ethyl and n-propyl.

Preferred aryl radicals which are optionally at least mono-substitutedare phenyl and naphthyl (1- and 2-naphthyl).

Preferably the heteroatoms which are present as ring members in theheteroaryl radical may, unless defined otherwise, independently beselected from the group consisting of nitrogen, oxygen and sulfur. Morepreferably a heteroaryl radical is 5- to 14-membered and may comprise 1,2, 3 or 4 heteroatoms independently selected from the group consistingof nitrogen, oxygen and sulfur.

Preferred heteroaryl radicals which are unsubstituted or at leastmono-substituted are pyridinyl, furyl (furanyl), thienyl (thiophenyl),pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyl,isoindolyl, pyrimidinyl, pyrazinyl, quinolinyl, isoquinolinyl,benzo[b]furanyl, benzo[b]thiophenyl, benzo[2,1,3]thiadiazolyl,[1,2,3]-benzothiadiazolyl, [2,1,3]-benzoxadiazolyl,[1,2,3]-benzoxadiazolyl, benzoxazolyl, benzthiazolyl, benzisoxazolyl,benzisothiazolyl, imidazo[2,1-b]thiazolyl, 2H-chromenyl, pyranyl,indazolyl and quinazolinyl.

Preferred aryl and heteroaryl radicals which are condensed with a mono-or polycyclic ring system are [1,3]-benzodioxolyl, [1,4]-benzodioxanyl,[1,2,3,4]-tetrahydronaphthyl, (2,3)-dihydro-1H-cyclopenta[b]indolyl,[1,2,3,4]-tetrahydroquinolinyl, [1,2,3,4]-tetrahydroisoquinolinyl,[1,2,3,4]-tetrahydroquinazolinyl and[3,4]-dihydro-2H-benzo[1,4]oxazinyl.

If one or more of the residues R¹ to R²² represents or comprises asaturated or unsaturated, optionally at least one heteroatom as a ringmember containing cycloaliphatic radical, preferably aC₃₋₁₈cycloaliphatic radical, a heterocyclic ring, preferably a 4- to 10-membered heterocyclic ring, a C₃₋₁₆cycloalkyl radical, aC₄₋₁₆cycloalkenyl radical, a C₄₋₁₆heterocycloalkyl radical, or aC₅₋₁₆heterocycloalkenyl radical, which may be substituted, unlessdefined otherwise, preferably said cycloaliphatic radical, heterocyclicring, C₃₋₁₆cycloalkyl radical, C₄₋₁₆cycloalkenyl radical,C₄₋₁₆heterocycloalkyl radical, or C₅₋₁₆heterocycloalkenyl radical, mayin each case optionally be substituted with 1, 2, 3, 4 or 5substituent(s) independently selected from the group consisting of oxo(═O), thioxo (═S), -C₁₋₆-perfluoralkyl, -C₁₋₆-alkyl, —C₁₋₆-alkylsubstituted with one or more hydroxy groups, —C₁₋₆-alkyl substitutedwith one or more chlorine atoms, —C₁₋₆-alkyl substituted with one ormore methoxy and/or ethoxy groups, —O—C₁₋₆-alkyl, -—O—C₁₋₆-alkylsubstituted with one or more methoxy and/or ethoxy groups,—S—C₁₋₆-alkyl, —C(═O)—OH, —C(═O)—O—C₁₋₆-alkyl, —O—C(═O)—C₁₋₆-alkyl, F,Cl, Br, I, —CN, —OCF₃, —O—C₂F₅, —O—C₃F₇, —O—C₄F₉, —SCF₃, —SCF₂H, —SCFH₂,—OH, —SH, —SO₃H, —NH—C(═O)—C₁₋₆-alkyl, —N(C₁₋₆-alkyl)—C(═O)—C₁₋₆-alkyl,—NO₂, —CHO, —C(═O)—C₁₋₆-alkyl, —C(═O)—C₁₋₆-perfluoroalkyl,—C(═S)—NH—C₁₋₆-alkyl, —CF₂H, —CFH₂, —C(═O)—NR^(A)R^(B),—C(═O)—NH—NR^(C)R^(D), —S(═O)—C₁₋₆-alkyl, —S(═O)₂-C₁₋₆-alkyl,—S(═O)₂-phenyl, —(C₁₋₅-alkylene)—S—C₁₋₆-alkyl,—(C₁₋₅-alkylene)—S(═O)—C₁₋₆-alkyl, —(C₁₋₅-alkylene)—S(═O)₂—C₁₋₆-alkyl,—NR^(E)R^(F), —(C₁₋₅-alkylene)—NR^(E)R^(F), —S(═O)—NH₂,—S(═O)₂—NH—C₁₋₆-alkyl, —S(═O)₂—NH-phenyl, —NH—S(═O)₂—C₁₋₆-alkyl,—O—Benzyl, —O—Phenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl,pyrrolidinyl, piperidinyl, phenyl, thiophenyl, phenoxy and benzyl;

whereby in each case the cyclic moieties cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, phenyl, thiophenyl,phenoxy and benzyl can optionally be-substituted with 1, 2, 3, 4 or 5substituent(s) independently selected from the group consisting of F,Cl, Br, I, —OH, —CF₃, —CN, —NO₂, —C₁₋₆-alkyl, —O—C₁₋₆-alkyl, —O—CF₃ and—S—CF₃ and

whereby R^(A), R^(B), R^(E) and R^(F), independently of one another,represent hydrogen or —C₁₋₆-alkyl or R^(A) and R^(B) in each casetogether with the bridging nitrogen atom form a radical selected fromthe group consisting of pyrrolidinyl, imidazolidinyl, piperazinyl,piperidinyl, thiomorpholinyl, morpholinyl, azepanyl and diazepanyl whichmay be at least mono-substituted with one or more identical or differentC₁₋₆-alkyl radicals

and whereby R^(C) and R^(D), independently of one another, representhydrogen, —C₁₋₆-alkyl, —C(═O)—O—C₁₋₆-alkyl, C₃₋₈-cycloalkyl,—(C₁₋₅-alkylene)—C₃₋₈-cycloalkyl, —(C₁₋₆-alkylene)—O—C₁₋₆-alkyl or—C₁₋₆-alkyl substituted with one or more hydroxy groups or R^(C) andR^(D) in each case together with the bridging nitrogen atom form aradical selected from-the group consisting of pyrrolidinyl,imidazolidinyl, piperazinyl, piperidinyl, thiomorpholinyl, morpholinyl,azepanyl and diazepanyl which may be at least mono-substituted with oneor more substituents independently selected from the group consisting—C₁₋₆-alkyl, —C(═O)—C₁₋₆-alkyl, —C(═O)—O—C₁₋₆-alkyl,—C(═O)—NH—C₁₋₆-alkyl, —C(═S)—NH—C₁₋₆-alkyl, oxo (═O), —C₁₋₆-alkylsubstituted with one or more hydroxy groups,—(C₁₋₆-alkylene)—O—C₁₋₆-alkyl and —C(═O)—NH₂.

More preferably said cycloaliphatic radicals, heterocyclic rings,C₃₋₁₆cycloalkyl radicals, C₄₋₁₆cycloalkenyl radicals,C₄₋₁₆heterocycloalkyl radicals, or C₅₋₁₆heterocycloalkenyl radicals, mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of oxo (═O), thioxo(═S), —CF₃, —C₂F₅, —C₃F₇, —C₄F₉, —CH₂Cl, —CHCl₂, —C₂H₄Cl, methyl, ethyl,n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,2-pentyl, n-hexyl, —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —O—CH₂—O—CH₃,—O—CH₂—CH₂—O—CH₃, —O—CH₂—O—C₂H₅, —C(OCH₃)(C₂H₅)₂, —C(OCH₃)(CH₃)₂,—O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃,—O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,—S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C₃H₇, —C(═O)—O—C(CH₃)₃, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅,—O—C(═O)—CH(CH₃)₂, —O—C(═O)—CH₂—CH₂—CH₃, —O—C(═O)—C(CH₃)₃, F, Cl, Br, I,—CN, —OCF₃, —O—C₂F₅, —O—C₃F₇, —O—C₄F₉, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH,—SO₃H, —NH—C(═O)—CH₃, —NH—C(═O)—C₂H₅, —NH—C(═O)—C(CH₃)₃, —NO₂, —CHO,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —C(═O)—CF₃, —C(═O)—C₂F₅,—C(═O)—C₃F₇, —C(═S)—NH—CH₃—C(═S)—NH—C₂H₅, —CF₂H, —CFH₂, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —C(═O)—NH—NH—CH₃, —C(═O)—NH—NH—C₂H₅, —C(═O)—NH—NH₂,—C(═O)—NH—N(CH₃)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,—S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —S(═O)₂-phenyl, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂, —N(C₂H₅)₂, —CH2—N(CH₃)₂, —(CH₂)-morpholinyl,—(CH₂)-piperidinyl, —(CH₂)-piperazinyl, —(CH₂)—N(C₂H₅)₂, —CH₂—N(C₃H₇)₂,—CH₂—N(C₄H₉)₂, —CH₂, —N(CH₃)(C₂H₅), —S(═O)—NH₂, —S(═O)₂—NH—CH₃,—S(═O)₂—NH-phenyl, —NH—S(═O)₂—CH₃, —O-Benzyl, —O-Phenyl, cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, phenyl,thiophenyl, phenoxy and benzyl, whereby said thiophenyl radical can besubstituted with 1, 2 or 3 substituents independently selected from thegroup consisting of F, Cl, Br, methyl, ethyl and n-propyl.

If one or more of the residues R¹ to R²² represents or comprises acycloaliphatic radical, preferably a C₃₋₁₆cycloaliphatic radical, whichcontains one or more heteroatoms as ring members, unless definedotherwise, each of these heteroatoms may preferably be selected from thegroup consisting of nitrogen, oxygen and sulfur. More preferably acycloaliphatic group may optionally contain 1, 2, 3 or 4 heteroatom(s)independently selected from the group consisting of N, O and S as ringmembers.

Suitable saturated or unsaturated, optionally at least one heteroatom asring member containing cycloaliphatic radicals may preferably beselected from the group consisting of cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl, cyclotetradecyl,cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, pyrrolidinyl,piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl,azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, azepanyl, diazepanyl, azocanyl,(2,5)-dihydrofuranyl, (2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl,(2,3)-dihydrofuranyl, (2,5)-dihydro-1H-pyrrolyl,(2,3)-dihydro-1H-pyrrolyl, tetrahydrothiopyranyl, tetrahydropyranyl,(3,4)-dihydro-2H-pyranyl, (3,4)-dihydro-2H-thiopyranyl,(1,2,3,6)-tetrahydropyridinyl, (1,2,3,4)-tetrahydropyridinyl,(1,2,5,6)-tetrahydropyridinyl, [1,3]-oxazinanyl, hexahydropyrimidinyl,(5,6)-dihydro-4H-pyrimidinyl, oxazolidinyl, (1,3)-dioxanyl,(1,4)-dioxanyl and (1,3)-dioxolanyl.

Suitable saturated or unsaturated, optionally at least one heteroatom asring member containing cycloaliphatic radicals which are condensed withan unsubstituted or at least mono-substituted mono- or polycyclic ringsystem may preferably be selected from the group consisting ofindolinyl, isoindolinyl, decahydronaphthyl,(1,2,3,4)-tetrahydroquinolinyl, (1,2,3,4)-tetrahydroisoquinolinyl,(1,2,3,4)-tetrahydronaphthyl, octahydro-cyclopenta[c]pyrrolyl,(1,3,4,7,9a)-hexahydro-2H-quinolizinyl,(1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,(6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,(2,3)-dihydro-1H-benzo[de]isoquinolinyl and (1,2,3,4)-tetrahydroquinoxazlinyl.

Preferably a cycloaliphatic radical, a C₁₋₆ cycloalkyl radical, a C₄₋₆cycloalkenyl radical, a C₄₋₆ heterocycloalkyl radical or a C₅₋₁₆heterocycloalkenyl radical may be bridged by 1, 2 or 3 unsubstituted orat least mono-substituted alkylene group(s).

Suitable saturated or unsaturated, optionally at least one heteroatom asring member containing cycloaliphatic radicals which are bridged by atleast one unsubstituted or at least mono-substituted alkylene group maypreferably be selected from the group consisting of adamantyl,bicyclo[2.2.1]heptyl, bicyclo[3.1.1]heptyl, norbornenyl and8-aza-bicyclo[3.2.1]octyl.

A suitable saturated or unsaturated, optionally at least one heteroatomas ring member containing cycloaliphatic radical which together with asaturated or unsaturated, unsubstituted or at least mono-substitutedcycloaliphatic radical forms a spirocyclic residue via a common ringatom is 8-aza-spiro[4.5]decanyl.

A mono- or polycyclic ring system according to the present invention—ifnot defined otherwise—means a mono- or polycyclic hydrocarbon ringsystem, preferably a mono- or bicyclic ring system, that may besaturated, unsaturated or aromatic. Each of its different rings may showa different degree of saturation, i.e. they may be saturated,unsaturated or aromatic. Optionally each of the rings of the mono- orbicyclic ring system may contain one or more, preferably 1, 2 or 3,heteroatom(s) as ring member(s), which may be identical or different andwhich can preferably be selected from the group consisting of nitrogen,oxygen and sulfur. The rings of the mono- or bicyclic ring system arepreferably 5-, 6- or 7-membered.

The term “condensed” according to the present invention means that aring or ring system is attached to another ring or ring system, wherebythe terms “annulated” or “annelated” are also used by those skilled inthe art to designate this kind of attachment.

If one or more of the residues R¹ to R²² comprises a mono- or polycyclicring system, which may be substituted, unless defined otherwise,preferably said mono- or polycyclic ring system may optionally besubstituted with 1, 2, 3, 4 or 5 substituent(s) independently selectedfrom the group consisting of oxo (═O), thioxo (═S), —C₁₋₆-perfluoralkyl,—C₁₋₆-alkyl, —C₁₋₆-alkyl substituted with one or more hydroxy groups,—C₁₋₆-alkyl substituted with one or more chlorine atoms, —C₁₋₆-alkylsubstituted with one or more methoxy and/or ethoxy groups,—O—C₁₋₆-alkyl, —O—C₁₋₆-alkyl substituted with one or more methoxy and/orethoxy groups, —S—C₁₋₆-alkyl, —C(═O)—OH, —C(═O)—O—C₁₋₆-alkyl,—O—C(═O)—C₁₋₆-alkyl, F, Cl, Br, I, —CN, —OCF₃, —O—C₂F₅, —O—C₃F₇,—O—C₄F₉, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —SO₃H, —NH—C(═O)—C₁₋₆-alkyl,—N(C₁₋₆-alkyl)—C(═O)—C₁₋₆-alkyl, —NO₂, —CHO, —C(═O)—C₁₋₆-alkyl,—C(═O)—C₁₋₆-perfluoroalkyl, —C(═S)—NH—C₁₋₆-alkyl, —CF₂H, —CFH₂,—C(═C)—NR^(A)R^(B), —C(═O)—NH—NR^(C)R^(D), —S(═O)—C₁₋₆-alkyl,—S(═C)₂—C₁₋₆-alkyl, —S(═O)₂-phenyl, —(C₁₋₅-alkylene)—S—C₁₋₆-alkyl,—(C₁₋₅-alkylene)—S(═O)—C₁₋₆-alkyl, —(C₁₋₅-alkylene)—S(═O)₂—C₁₋₆-alkyl,—NR^(E)R^(F), —(C₁₋₅alkylene)—NR^(E)R^(F), —S(═O)—NH₂,—S(═O)₂—NH—C₁₋₆-alkyl, —S(═O)₂—NH-phenyl, —NH—S(═O)₂—C₁₋₆-alkyl,cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, pyrrolidinyl,piperidinyl, phenyl, thiophenyl, phenoxy and benzyl;

whereby in each case the cyclic moieties cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, phenyl, thiophenyl,phenoxy and benzyl can optionally be substituted with 1, 2, 3, 4 or 5substituent(s) independently selected from the group consisting of F,Cl, Br, I, —OH, —CF₃, —CN, —NO₂, —C₁₋₆-alkyl, —O—C₁₋₆-alkyl, —O—CF₃ and—S—CF₃ and

whereby R^(A), R^(B), R^(E) and R^(F), independently of one another,represent hydrogen or —C₁₋₆-alkyl or R^(A) and R^(B) in each casetogether with the bridging nitrogen atom form a radical selected fromthe group consisting of pyrrolidinyl, imidazolidinyl, piperazinyl,piperidinyl, thiomorpholinyl, morpholinyl, azepanyl and diazepanyl whichmay be at least mono-substituted with one or more identical or differentC₁₋₆-alkyl radicals

and whereby R^(C) and R^(D), independently of one another, representhydrogen, —C₁₋₆-alkyl, —C(═O)—O—C₁₋₆-alkyl, C₃₋₈-cycloalkyl,—(C₁₋₅-alkylene)—C₃₋₈-cycloalkyl, —(C₁₋₆-alkylene)—O—C₁₋₆-alkyl or—C₁₋₆-alkyl substituted with one or more hydroxy groups or R^(C) andR^(D) in each case together with the bridging nitrogen atom form aradical selected from the group consisting of pyrrolidinyl,imidazolidinyl, piperazinyl, piperidinyl, thiomorpholinyl, morpholinyl,azepanyl and diazepanyl which may be at least mono-substituted with oneor more substituents independently selected from the group consisting—C₁₋₆-alkyl, —C(═O)—C₁₋₆-alkyl, —C(═O)—O—C₁₋₆-alkyl,—C(═O)—NH—C₁₋₆-alkyl, —C(═S)—NH—C₁₋₆-alkyl, oxo (═O), —C₁₋₆-alkylsubstituted with one or more hydroxy groups,—(C₁₋₆-alkylene)—O—C₁₋₆-alkyl and —C(═O)—NH₂.

More preferably said mono- or polycyclic ring system may optionally besubstituted with 1, 2, 3, 4 or 5 substituent(s) independently selectedfrom the group consisting of oxo (═O), thioxo (═S), —CF₃, —C₂F₅, —C₃F₇,—C₄F₉, —CH₂Cl, —CHCl₂, —C₂H₄Cl, methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,—CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —O—CH₂—O—CH₃, —O—CH₂—CH₂—O—CH₃,—O—CH₂—O—C₂H₅, —C(OCH₃)(C₂H₅)₂, —C(OCH₃)(CH₃)₂, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,—S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃,—C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C₃H₇, —C(═O)—O—C(CH₃)₃,—O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂, —O—C(═O)—CH₂—CH₂—CH₃,—O—C(═O)—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —O—C₂F₅, —O—C₃F₇, —O—C₄F₉,—SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —SO₃H, —NH—C(═O)—CH₃, —NH—C(═O)—C₂H₅,—NH—C(═O)—C(CH₃)₃, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃,—C(═O)—CF₃, —C(═O)—C₂F₅, —C(═O)—C₃F₇, —C(═S)—NH—CH₃, —C(═S)—NH—C₂H₅,—CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH-CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —C(═O)—NH—NH—CH₃, —C(═O)—NH—NH—C₂H₅,—C(═O)—NH—NH₂, —C(═O)—NH—N(CH₃)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂-phenyl, —NH₂, —NH—CH₃,—NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —CH₂—N(CH₃)₂, —(CH₂)-morpholinyl,—(CH₂)—piperidinyl, —(CH₂)-piperazinyl, —(CH₂)—N(C₂H₅)₂, —CH₂—N(C₃H₇)₂,—CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅), —S(═O)—NH₂, —S(═O)₂—NH—CH₃,—S(═O)₂—NH-phenyl, —NH—S(═O)₂—CH₃, cyclopropyl, cyclobutyl, cyclopentyl,cyclohexyl, pyrrolidinyl, piperidinyl, phenyl, thiophenyl, phenoxy andbenzyl, whereby said thiophenyl radical can be substituted with 1, 2 or3 substituents independently selected from the group consisting of F,Cl, Br, methyl, ethyl and n-propyl.

If one or more of the residues R⁴ to R²² represent or comprise asaturated or unsaturated, unsubstituted or at least mono-substitutedaliphatic radical, preferably a C₁₋₆aliphatic radical, said aliphaticradical may be linear or branched.

Preferably aliphatic radicals, C₁₋₆-alkyl radicals, C₂ ₁₆alkenyl radicaland C₂₋₁₆alkinyl radicals, unless defined otherwise, may optionally besubstituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents independentlyselected from the group consisting of —OH, F, Cl, Br, I, —O—C₁₋₆-alkyl,—OCF₃, —O—C₂F₅, —O—C₃F₇, —O—C₄F₉, —CF₃, —C₂F₅, —C₃F₇, —C₄F₉, —NH₂,—NH—C₁₋₆-alkyl, —N(C₁₋₆-alkyl)₂, —C(═O)—OH, —C(═O)—O—C₁₋₆-alkyl,—C(═O)—NH₂, —C(═O)—NH—C₁₋₆-alkyl, —C(═O)—N(C₁₋₆-alkyl)₂, —CN, —NO₂,—S(═O)—NH₂, —CHO, —C(═O)—C₁₋₆-alkyl, —S(═O)—C₁₋₆-alkyl,—S(═O)₂—C₁₋₆-alkyl, —NH—S(═O)—C₁₋₆-alkyl, —NH—C(═O)—O—C₁₋₆-alkyl and—NH—C(═O)—C₁₋₆-alkyl.

More preferably aliphatic radicals, C₁₋₆-alkyl radicals, C₂₋₁₆alkenylradical and C₂₋₁₆alkinyl radicals may optionally be substituted with 1,2, 3, 4, 5, 6, 7, 8 or 9 substituents independently selected frorn thegroup consisting of —OH F, Cl, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,—O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂, —N(C₂H₅)₂, —CN, —NO₂, —NH—C(═O)—CH₃, —NH—C(═O)—C₂H₅,—NH—C(═O)—C(CH₃)₃, —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅,—NH—C(═O)—O—C(CH₃)₃, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C(CH₃)₃,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅ and —C(═O)—C(CH₃)₃.

Suitable alkyl radicals, preferably C₁₋₆-alkyl radicals, are selectedfrom the group consisting of methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl,neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl,4-heptyl, n-octyl, 2-octyl, 3-octyl, 4-octyl, 2-(6-methyl)-heptyl,2-(5-methyl)-heptyl, 2-(5-methyl)-hexyl, 2-(4-methyl)-hexyl,2-(7-methyl)-octyl, 2-(6-methyl)-octyl, n-nonyl, n-decyl, n-undecyl,n-dodecyl, n-tridecyl, n-tetradecyl, n-pentadecycl and n-hexadecyl

Suitable at least mono-substituted alkyl radicals are selected from thegroup consisting of -CF₃, —CH₂F, —CF₂H, —CH₂—O—CH₃, —C₂F₅, —CH₂—CH₂—F,—CH₂—CN, —CH₂—OH, —CH₂—CH₂—CN, —CH₂—CH₂—OH, —CH₂—CH₂—OCH₃,—CH₂—CH₂—CH₂—CN, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—O—CH₃,—CH₂—CH₂—CH₂—CH₂—O—CH₃, —CH₂—NH₂, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂,—CH₂—CH—NH₂, —CH₂—CH₂—N(CH₃)₂, —CH₂—CH₂—N(C₂H₅)₂, —CH₂—CH₂—CH₂—NH₂,—CH₂—CH₂—CH₂—N(CH₃)₂ and —CH₂—CH₂—CH₂—N(C₂H₅)₂.

An alkenyl radical according to the present invention comprises at leastone carbon-carbon double bond. Suitable alkenyl radicals, preferablyC₂₋₁₆ alkenyl radicals, are selected from the group consisting of vinyl,n-propenyl, n-butenyl, n-pentenyl, n-hexenyl, n-heptenyl, n-octenyl,n-nonenyl, n decenyl, n-undecenyl, n-dodecenyl, n-tridecenyl,n-tetradecenyl, n-pentadecenyl and n-hexadecenyl.

An alkinyl radical comprises at least one carbon-carbon triple bond.Suitable alkinyl radicals, preferably C₂-₁₆alkinyl radicals, areselected from the group consisting of ethinyl, propinyl, n-butinyl,n-pentinyl, n-hexinyl, n-octinyl, n-noninyl, n-decinyl, n-undecinyl,n-dodecinyl, n-tridecinyl, n-tetradecinyl, n-pentadecinyl andn-hexadecinyl.

If any of the substituents represents an alkylene group, an alkenylenegroup or an alkinylene group, which may be substituted, said alkylenegroup, alkenylene group or alkinylene group may—if not definedotherwise—be unsubstituted or substituted by one or more substituents,preferably unsubstituted or substituted with 1, 2 or 3 substituent(s).Said substituent(s) may preferably be selected independently from thegroup consisting of —O—C₁₋₆-alkyl, —S—C₁₋₆-alkyl, —F, Cl, Br, I, —CN,—CF₃, —OCF₃, —SCF₃, —OH, —SH, —SO₃H, —NH₂, —NH(C₁₋₆-alkyl),—N(C₁₋₆-alkyl)₂ and phenyl. More preferably said substituent(s) may beselected from the group consisting of —F, Cl, Br, I, —CN, —CF₃, —OCF₃,—SCF₃, —OH, —SH, —SO₃H, —NH₂, —NH—CH₃, —N(CH₃)₂, —O—CH₃ and —O—C₂H₅. Analkenylene group comprises at least one carbon-carbon double bond, analkinylene group comprises at least one carbon-carbon triple bond.

Suitable alkylene groups, preferably C₁₋₅-alkylene groups, include—(CH₂)—, —CH(CH₃)—, —CH(phenyl), —(CH₂)₂—, —(CH₂)₃—, —(CH₂)₄—, —(CH₂)₅and —(CH₂)₆—, suitable alkenylene groups, preferably C₂₋₅-alkenylenegroups, include —CH═CH—, —CH₂—CH—CH— and —CH—CH—CH₂— and suitablealkinylene groups, preferably C₂₋₅-alkinylene groups, include —C≡C—,—CH₂—C≡C— and —C≡C—CH₂—.

Preferred are 4-substituted pyrazoline compounds of general formula Igiven above, wherein

-   x is O or S;-   R¹ and R², independently of one another, in each case represent an    unsubstituted or at least mono-substituted 6- or 10-membered aryl    radical, which may be condensed with an unsubstituted or at least    mono-substituted mono- or polycyclic ring system;-   an unsubstituted or at least mono-substituted 5- to 14-membered    heteroaryl radical, which may be condensed with an unsubstituted or    at least mono-substituted mono- or polycyclic ring system;-   an unsubstituted or at least mono-substituted C₃₋₁₆cycloalkyl    radical or C₄₋₁₆cycloalkenyl radical, which in each case may be    condensed with an unsubstituted or at least mono-substituted mono-    or polycyclic ring system and/or may be bridged by at least one    unsubstituted or at least mono-substituted C₁₋₅alkylene group;-   or an unsubstituted or at least mono-substituted    C₄₋₁₆heterocycloalkyl radical or C₅₋₁₆heterocycloalkenyl radical,    which in each case may be condensed with an unsubstituted or at    least mono-substituted mono- or polycyclic ring system and/or may be    bridged by at least one unsubstituted or at least mono-substituted    C₁₋₅alkylene group;-   R³ represents an unsubstituted or at least mono-substituted 6- or    10-membered aryl radical, which may be condensed with an    unsubstituted or at least mono-substituted mono- or polycyclic ring    system;-   an unsubstituted or at least mono-substituted 5- to 14-membered    heteroaryl radical, which may be condensed with an unsubstituted or    at least mono-substituted mono- or polycyclic ring system;-   an unsubstituted or at least mono-substituted C₃₋₁₆cycloalkyl    radical or C₄₋₁₆cycloalkenyl radical, which in each case may be    condensed with an unsubstituted or at least mono-substituted mono-    or polycyclic ring system and/or may be bridged by at least one    unsubstituted or at least mono-substituted C₁₋₅alkylene group;-   an unsubstituted or at least mono-substituted C₄₋₁₆heterocycloalkyl    radical or C₅₋₁₆heterocycloalkenyl radical, which in each case may    be condensed with an unsubstituted or at least mono-substituted    mono- or polycyclic ring system and/or may be bridged by at least    one unsubstituted or at least mono-substituted C₁₋₅alkylene group;-   an unsubstituted or at least mono-substituted C₃₋₁₆cycloalkyl    radical, C₄₋₁₆cycloalkenyl radical, C₄₋₁₆heterocycloalkyl radical or    C₅₋₁₆heterocycloalkenyl radical which together with an unsubstituted    or at least mono-substituted C₃₋₁₆cycloalkyl radical,    C₄₋₁₆cycloalkenyl radical, C₄₋₁₆heterocycloalkyl radical or    C₅₋₁₆heterocycloalkenyl radical forms an unsubstituted or at least    mono-substituted spirocyclic residue via a common ring atom;-   a —O—R⁶ moiety; a —NR⁷R⁸ moiety or a —NR⁹—O—R¹⁰ moiety;-   R⁴ represents F; Cl; Br; I; —CN; —NO₂; —NC; —OH; —NH₂; —SH;    —C(═O)—H; —C(═O)—OH; —C(═O)—OR¹⁷;-   an unsubstituted or at least mono-substituted C₁₋₁₆alkyl radical,    C₂₋₁₆alkenyl radical or C₂₋₁₆alkinyl radical;-   an unsubstituted or at least mono-substituted C₃₋₁₆cycloalkyl    radical or C₄₋₁₆cycloalkenyl radical, which in each case may be    condensed with an unsubstituted or at least mono-substituted mono-    or polycyclic ring system and/or may be bonded via an unsubstituted    or at least mono-substituted C₁₋₅alkylene group, C₂₋₅alkenylene    group or C₂₋₅alkinylene group and/or may be bridged by at least one    unsubstituted or at least mono-substituted C₁₋₅alkylene group;-   an unsubstituted or at least mono-substituted C₄₋₁₆heterocycloalkyl    radical or C₅₋₁₆heterocycloalkenyl radical, which in each case may    be condensed with an unsubstituted or at least mono-substituted    mono- or polycyclic ring system and/or may be bonded via an    unsubstituted or at least mono-substituted C₁₋₅alkylene group,    C₂₋₅alkenylene group or C₂₋₅alkinylene group and/or may be bridged    by at least one unsubstituted or at least mono-substituted    C₁₋₅alkylene group;-   an unsubstituted or at least mono-substituted 6- or 10-membered aryl    radical, which may be condensed with an unsubstituted or at least    mono-substituted mono- or polycyclic ring system and/or may be    bonded via an unsubstituted or at least mono-substituted    C₁₋₅alkylene group, C₂₋₅alkenylene group or C₂₋₅alkinylene group;-   or an unsubstituted or at least mono-substituted 5- to 14-membered    heteroaryl radical, which may be condensed with an unsubstituted or    at least mono-substituted mono- or polycyclic ring system and/or may    be bonded via an unsubstituted or at least mono-substituted    C₁₋₅alkylene group, C₂₋₅alkenylene group or C₂₋₅alkinylene group;-   a —O—R¹¹ moiety; a —S—R¹² moiety; a —NH—R¹³ moiety or a —NR¹⁴R¹⁵    moiety;-   R⁵ represents H; F; Cl; Br; I; —CN; —NO₂; —NC; —OH; —NH₂; —SH;    —C(═O)—H; —C(═O)—OH; —C(═O)—OR¹⁷;-   an unsubstituted or at least mono-substituted C₁₋₆alkyl radical,    C₂₋₁₆alkenyl radical or C₂₋₁₆alkinyl radical;-   an unsubstituted or at least mono-substituted C₃₋₁₆cycloalkyl    radical or C₄₋₁₆cycloalkenyl radical, which in each case may be    condensed with an unsubstituted or at least mono-substituted mono-    or polycyclic ring system and/or may be bonded via an unsubstituted    or at least mono-substituted C₁₋₅alkylene group, C₂₋₅alkenylene    group or C₂₋₅alkinylene group and/or may be bridged by at least one    unsubstituted or at least mono-substituted C₁₋₅alkylene group;-   an unsubstituted or at least mono-substituted C₄₋₁₆heterocycloalkyl    radical or C₅₋₁₆heterocycloalkenyl radical, which in each case may    be condensed with an unsubstituted or at least mono-substituted    mono- or polycyclic ring system and/or may be bonded via an    unsubstituted or at least mono-substituted C₁₋₅alkylene group,    C₂₋₅alkenylene group or C₂₋₅alkinylene group and/or may be bridged    by at least one unsubstituted or at least mono-substituted    C₁₋₅alkylene group;-   an unsubstituted or at least mono-substituted 6- or 10-membered aryl    radical, which may be condensed with an unsubstituted or at least    mono-substituted mono- or polycyclic ring system and/or may be    bonded via an unsubstituted or at least mono-substituted    C₁₋₅alkylene group, C₂₋₅alkenylene group or C₂₋₅alkinylene group;-   or an unsubstituted or at least mono-substituted 5- to 14-membered    heteroaryl radical, which may be condensed with an unsubstituted or    at least mono-substituted mono- or polycyclic ring system and/or may    be bonded via an unsubstituted or at least mono-substituted    C₁₋₅alkylene group, C₂₋₅alkenylene group or C₂₋₅alkinylene group;-   —O—R¹¹ moiety; a —S—R¹² moiety; a —NH—R¹³ moiety or a —NR¹⁴R¹⁵    moiety;-   or R⁴ and R⁵ together with the bridging carbon atom form an    unsubstituted or at least mono-substituted C₃₋₁₆cycloalkyl radical    or C₄₋₁₆cycloalkenyl radical;-   R⁶ represents a hydrogen atom;-   an unsubstituted or at least mono-substituted C₁₋₁₆alkyl radical,    C₂₋₁₆alkenyl radical or C₂₋₁₆alkinyl radical;-   an unsubstituted or at least mono-substituted C₃₋₁₆cycloalkyl    radical or C₄₋₁₆cycloalkenyl radical, which in each case may be    condensed with an unsubstituted or at least mono-substituted mono-    or polycyclic ring system and/or may be bridged by at least one    unsubstituted or at least mono-substituted C₁₋₅alkylene group and/or    may be bonded via an unsubstituted or at least mono-substituted    C₁₋₅alkylene group, C₂₋₅alkenylene group or C₂₋₅alkinylene group;-   an unsubstituted or at least mono-substituted C₄₋₁₆heterocycloalkyl    radical or C₅₋₁₆heterocycloalkenyl radical, which in each case may    be condensed with an unsubstituted or at least mono-substituted    mono- or polycyclic ring system and/or may be bridged by at least    one unsubstituted or at least mono-substituted C₁₋₅alkylene group    and/or may be bonded via an unsubstituted or at least    mono-substituted C₁₋₅alkylene group, C₂₋₅alkenylene group or    C₂₋₅alkinylene group;-   an unsubstituted or at least mono-substituted 6- or 10-membered aryl    radical, which may be condensed with an unsubstituted or at least    mono-substituted mono- or polycyclic ring system and/or may be    bonded via an unsubstituted or at least mono-substituted    C₁₋₅alkylene group, C₂₋₅alkenylene group or C₂₋₅alkinylene group;-   an unsubstituted or at least mono-substituted 5- to 14-membered    heteroaryl radical, which may be condensed with an unsubstituted or    at least mono-substituted mono- or polycyclic ring system and/or may    be bonded via an unsubstituted or at least mono-substituted    C₁₋₅alkylene group, C₂₋₅alkenylene group or C₂₋₅alkinylene group;-   a —P(═O)(OR¹⁶)₂ moiety; a —C(═O)—OR¹⁷ moiety; a —C(═O)—NH—R¹⁸ moiety    or a —C(═O)—R¹⁹ moiety;-   R⁷ and R⁸, independently of one another, in each case represent a    hydrogen atom;-   an unsubstituted or at least mono-substituted C₁₋₁₆alkyl radical,    C₂₋₁₆alkenyl radical or C₂₋₁₆alkinyl radical;-   an unsubstituted or at least mono-substituted C₃₋₁₆cycloalkyl    radical or C₄₋₁₆cycloalkenyl radical, which in each case may be    condensed with an unsubstituted or at least mono-substituted mono-    or polycyclic ring system and/or may be bridged by at least one    unsubstituted or at least mono-substituted C₁₋₅alkylene group and/or    may be bonded via an unsubstituted or at least mono-substituted    C₁₋₅alkylene group, C₂₋₅alkenylene group or C₂₋₅alkinylene group;-   an unsubstituted or at least mono-substituted C₄₋₁₆heterocycloalkyl    radical or C₅₋₁₆heterocycloalkenyl radical, which in each case may    be condensed with an unsubstituted or at least mono-substituted    mono- or polycyclic ring system and/or may be bridged by at least    one unsubstituted or at least mono-substituted C₁₋₅alkylene group    and/or may be bonded via an unsubstituted or at least    mono-substituted C₁₋₅alkylene group, C₂₋₅alkenylene group or    C₂₋₅alkinylene group;-   an unsubstituted or at least mono-substituted C₃₋₁₆cycloalkyl    radical, C₄₋₁₆cycloalkenyl radical, C₄₋₁₆heterocycloalkyl radical or    C₅₋₁₆heterocycloalkenyl radical which together with an unsubstituted    or at least mono-substituted C₃₋₁₆cycloalkyl radical,    C₄₋₁₆cycloalkenyl radical, C₄₋₁₆heterocycloalkyl radical or    C₅₋₁₆heterocycloalkenyl radical forms an unsubstituted or at least    mono-substituted spirocyclic residue via a common ring atom;-   an unsubstituted or at least mono-substituted 6 or 10-membered aryl    radical, which may be condensed with an unsubstituted or at least    mono-substituted mono- or polycyclic ring system and/or may be    bonded via an unsubstituted or at least mono-substituted    C₁₋₅alkylene group, C₂₋₅alkenylene group or C₂₋₅alkinylene group;-   an unsubstituted or at least mono-substituted 5- to 14-membered    heteroaryl radical, which may be condensed with an unsubstituted or    at least mono-substituted mono- or polycyclic ring system and/or may    be bonded via an unsubstituted or at least mono-substituted    C₁₋₅alkylene group, C₂₋₅alkenylene group or C₂₋₅alkinylene group;-   a —P(═O)(OR¹⁶)₂ moiety; a —C(═O)—OR¹⁷ moiety; a —C(═O)—NH—R¹⁸    moiety; a —C(═O)—R¹⁹ moiety; a —S(═O)₂—R²⁰ moiety; or a —NR²¹R²²    moiety;-   R⁹ represents a hydrogen atom or an unsubstituted or at least    mono-substituted C₁₋₁₆alkyl radical, C₂₋₁₆alkenyl radical or    C₂₋₁₆alkinyl radical;-   R¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²⁰, independently of one another,    in each case represent an unsubstituted or at least mono-Substituted    C₁₋₁₆alkyl radical, C₂₋₁₆ alkenyl radical or C₂₋₁₆ alkinyl radical;-   an unsubstituted or at least mono-substituted C₃₋₁₆ cycloalkyl    radical or C₄₋₁₆ cycloalkenyl radical, which in each case may be    condensed with an unsubstituted or at least mono-substituted mono-    or polycyclic ring system and/or may be bridged by at least one    unsubstituted or at least mono-substituted C₁₋₅ alkylene group-    and/or may be bonded via an unsubstituted or at least    mono-substituted C₁₋₅ alkylene group, C₂₋₅ alkenylene group or C₂₋₅    alkinylene group;-   an unsubstituted or at least mono-substituted C₄₋₁₆ heterocycloalkyl    radical or C₅₋₁₆ heterocycloalkenyl radical, which in each case may    be condensed with an unsubstituted or at least mono-substituted    mono- or polycyclic ring system and/or may be bridged by at least    one unsubstituted or at least mono-substituted C₁₋₅ alkylene group    and/or may be bonded via-an unsubstituted or at least    mono-substituted C₁₋₅ alkylene group, C₂₋₅ alkenylene group or C₂₋₅    alkinylene group; an unsubstituted or at least mono-substituted 6 or    10-membered aryl radical, which may be condensed with an    unsubstituted or at least mono-substituted mono- or polycyclic ring    system and/or may be bonded via an unsubstituted or at least    mono-substituted C₁₋₅ alkylene group, C₂₋₅ alkenylene group or C₂₋₅    alkinylene group;-   or an unsubstituted or at least mono-substituted 5- to 14-membered    heteroaryl radical, which may be condensed with an unsubstituted or    at least mono-substituted mono- or polycyclic ring system and/or may    be bonded via an unsubstituted or at least mono-substituted C₁₋₅    alkylene group, C₂₋₅ alkenylene group or C₂₋₅ alkinylene group;-   R¹⁶, R¹⁷, R¹⁸ and R¹⁹, independently of one another, in each case    represent an unsubstituted or at least mono-substituted C₁₋₁₆ alkyl    radical, C₂₋₁₆ alkenyl radical or C₂₋₁₆ alkinyl radical;-   or an unsubstituted or at least mono-substituted 6 or 10-membered    aryl radical, which may be condensed with an unsubstituted or at    least mono-substituted mono- or polycyclic ring system and/or may be    bonded via an unsubstituted or at least mono-substituted C₁₋₅    alkylene group, C₂₋₅ alkenylene group or C₂₋₅ alkinylene group;-   or an unsubstituted or at least mono-substituted 5- to 14-membered    heteroaryl radical, which may be condensed with an unsubstituted or    at least mono-substituted mono- or polycyclic ring system and/or may    be bonded via an unsubstituted or at least mono-substituted C₁₋₅    alkylene group, C₂₋₅ alkenylene group or C₂₋₅ alkinylene group;    and-   R²¹ and R²², independently of one another, in each case represent a    hydrogen atom;-   an unsubstituted or at least mono-substituted C₁₋₆ alkyl radical,    C₂₋₁₆ alkenyl radical or C₂₋₁₆ alkinyl radical;-   an unsubstituted or at least mono-substituted C₃₋₁₆ cycloalkyl    radical or C₄₋₁₆ cycloalkenyl radical, which in each case may be    condensed with an unsubstituted or at least mono-substituted mono-    or polycyclic ring system and/or may be bonded via an unsubstituted    or at least mono-substituted C₁₋₅ alkylene group, C₂₋₅ alkenylene    group or C₂₋₅ alkinylene group;-   an unsubstituted or at least mono-substituted C₄₋₁₆ heterocycloalkyl    radical or C₅₋₁₆ heterocycloalkenyl radical, which in each case may    be condensed with an unsubstituted or at least mono-substituted    mono- or polycyclic ring system and/or may be bonded via an    unsubstituted or at least mono-substituted C₁₋₅ alkylene group, C₂₋₅    alkenylene group or C₂₋₅ alkinylene group;-   an unsubstituted or at least mono-substituted C₃₋₁₆ cycloalkyl    radical, C₄₋₁₆ cycloalkenyl radical, C₄₋₁₆ heterocycloalkyl radical    or C₅₋₁₆ heterocycloalkenyl radical which together with an    unsubstituted or at least mono-substituted C₃₋₁₆ cycloalkyl radical,    C₄₋₁₆ cycloalkenyl radical, C₄₋₁₆ heterocycloalkyl radical or C₅₋₁₆    heterocycloalkenyl radical forms an unsubstituted or at least    mono-substituted spirocyclic residue via a common ring atom;-   an unsubstituted or at least mono-substituted 6- or 10-membered aryl    radical, which may be condensed with an unsubstituted or at least    mono-substituted mono- or polycyclic ring system and/or may be    bonded via an unsubstituted or at least mono-substituted C₁₋₅    alkylene group, C₂₋₅ alkenylene group or C₂₋₅ alkinylene group;-   or an unsubstituted or at least mono-substituted 5- to 14-membered    heteroaryl radical, which may be condensed with an unsubstituted or    at least mono-substituted mono- or polycyclic ring system and/or may    be bonded via an unsubstituted or at least mono-substituted C₁₋₅    alkylene group, C₂₋₅ alkenylene group or C₂₋₅ alkinylene group;    whereby-   the rings of the aforementioned ring system are in each case    independently of one another 5- 6- or 7-membered and may in each    case independently of one another optionally contain 1, 2 or 3    heteroatom(s) independently selected from the group consisting of    nitrogen, oxygen and sulfur;-   the aforementioned heteroaryl radicals in each case optionally    contain 1, 2, 3 or 4 heteroatom(s) independently selected from the    group consisting of nitrogen, oxygen and sulfur as ring member(s);-   the aforementioned heterocycloalkyl radicals and heterocycloalkenyl    radicals in each case optionally contain 1, 2, 3 or 4 heteroatom(s)    independently selected from the group consisting of nitrogen, oxygen    and sulfur as ring member(s);-   optionally in form of one of its stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of its stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a physiologically acceptable salt thereof, or a    corresponding solvate thereof.

Also preferred are 4-substituted pyrazoline compounds of general formulaI given above, wherein R¹ and R², independently of one another, in eachcase represent a radical selected from the group consisting of phenyl,naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl,oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyl, isoindolyl,pyrimidinyl, pyrazinyl, quinolinyl, isoquinolinyl, benzo[b]furanyl,benzo[b]thiophenyl, benzo[2,1,3]thiadiazolyl, [1,2,3]-benzothiadiazolyl,[2,1,3]-benzoxadiazolyl, [1,2,3]-benzoxadiazolyl, benzoxazolyl,benzthiazolyl, benzisoxazolyl, benzisothiazolyl,imidazo[2,1-b]thiazolyl, 2H-chromenyl, pyranyl, indazolyl, quinazolinyl,[1,3]-benzodioxolyl, [1,4]-benzodioxanyl, [1,2,3,4]-tetrahydronaphthyl,(2,3)-dihydro-1H-cyclopenta[b]indolyl, [1,2,3,4]-tetrahydroquinolinyl,[1,2,3,4]-tetrahydroisoquinolinyl, [1,2,3,4]-tetrahydroquinazolinyl and[3,4]-dihydro-2H-benzo[1,4]oxazinyl, which in each case is optionallybonded to the pyrazoline compound of general formula I via the aromaticor heteroaromatic part of the aforementioned radicals and may optionallybe substituted with 1, 2, 3, 4 or 5 substituent(s) independentlyselected from the group consisting of —CF₃, —CH₂—Cl, methyl, ethyl,n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃,—S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃,—SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅,—C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃,—S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, phenoxy and thiophenyl, wherebythe thiophenyl radical can be substituted with 1, 2 or 3 substituentsindependently selected from the group consisting of F, Cl, Br, methyl,ethyl and n-propyl;

-   or a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl,    cyclotetradecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl, diazepanyl, azocanyl,    (2,5)-dihydrofuranyl, (2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl,    (2,3)-dihydrofuranyl, (2,5)-dihydro-1H-pyrrolyl,    (2,3)-dihydro-1H-pyrrolyl, tetrahydrothiopyranyl, tetrahydropyranyl,    (3,4)-dihydro-2H-pyranyl, (3,4)-dihydro-2H-thiopyranyl,    (1,2,3,6)-tetrahydropyridinyl, (1,2,3,4)-tetrahydropyridinyl,    (1,2,5,6)-tetrahydropyridinyl, [1,3]-oxazinanyl,    hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl, oxazolidinyl,    (1,3)-dioxanyl, (1,4)-dioxanyl, (1,3)-dioxolanyl, indolinyl,    isoindolinyl, decahydronaphthyl, (1,2,3,4)-tetrahydroquinolinyl,    (1,2,3,4)-tetrahydroisoquinolinyl, octahydro-cyclopenta[c]pyrrolyl,    (1,3,4,7,9a)-hexahydro-2H-quinolizinyl,    (1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,    dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,    (6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,    (2,3)-dihydro-1H-benzo[de]isoquinolinyl,    (1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,    bicyclo[3.1.1]heptyl and norbornenyl, which in each case is    optionally bonded to the pyrazoline compound of general formula I    via the (hetero)cycloaliphatic part of the aforementioned radicals    and may optionally be substituted with 1, 2, 3, 4 or 5    substituent(s) independently selected from the group consisting of    oxo (═0), thioxo (═S), —CF₃, methyl, ethyl, n-propyl, isopropyl,    n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,    —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃,    —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,    —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃,    —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,    —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃,    —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,    —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅,    —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂;-   and X and R³ to R² have the meaning given above, optionally in form    of one of the stereoisomers, preferably enantiomers or    diastereomers, a racemate or in form of a mixture of at least two of    the stereoisomers, preferably enantiomers and/or diastereomers, in    any mixing ratio, or a corresponding N-oxide thereof, or a    corresponding salt thereof, or a corresponding solvate thereof.

Preference is also given to 4-substituted pyrazoline compounds ofgeneral formula I given above, wherein R³ represents a radical selectedfrom the group consisting of (2,3)-dihydro-1H-cyclopenta[b]indolyl,cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl,cyclooctyl, cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl,cyclotridecyl, cyclotetradecyl, cyclopentenyl, cyclohexenyl,cycloheptenyl, cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl,thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl,azepanyl, diazepanyl, azocanyl, (2,5)-dihydrofuranyl,(2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl, (2,3)-dihydrofuranyl,(2,5)-dihydro-1H-pyrrolyl, (2,3)-dihydro-1H-pyrrolyl,tetrahydrothiopyranyl, tetrahydropyranyl, (3,4)-dihydro-2H-pyranyl,(3,4)-dihydro-2H-thiopyranyl, (1,2,3,6)-tetrahydropyridinyl,(1,2,3,4)-tetrahydropyridinyl, (1,2,5,6)-tetrahydropyridinyl,[1,3]-oxazinanyl, hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl,oxazolidinyl, (1,3)-dioxanyl, (1,4)-dioxanyl, (1,3)-dioxolanyl,indolinyl, isoindolinyl, decahydronaphthyl,(1,2,3,4)-tetrahydroquinolinyl, (1,2,3,4)-tetrahydroisoquinolinyl,octahydro-cyclopenta[c]pyrrolyl, (1,3,4,7,9a)-hexahydro-2H-quinolizinyl,(1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,dodecahydro—Carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,(6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,(2,3)-dihydro-1H-benzo[de]isoquinolinyl,(1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,bicyclo[3.1.1]heptyl, norbornenyl, 8-aza-bicyclo[3.2.1]octyl and8-aza-spiro[4.5]decanyl, which may optionally be substituted with 1, 2,3, 4 or 5 substituent(s) independently selected from the groupconsisting of oxo (═O), thioxo (═S), —CF₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl,n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —O—CH₂—O—CH₃, —O—CH₂—CH₂O—CH₃,—O—CH₂—O—C₂H₅, —C(OCH₃)(C₂H₅)₂, —C(OCH₃)(CH₃)₂, —S—CH₃, —S—C₂H₅,—S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br,I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(—O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃,—C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,—S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅,—S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, cyclopentyl,—O—Benzyl, benzyl, cyclohexyl, pyrrolidinyl and piperidinyl;

-   a —O—R⁶ moiety; a —NR⁷R⁸ moiety or a —NR⁹—O—R¹⁰ moiety;-   and X, R¹, R² and R⁴ to R²² have the meaning given above, optionally    in form of one of the stereoisomers, preferably enantiomers or    diastereomers, a racemate or in form of a mixture of at least two of    the stereoisomers, preferably enantiomers and/or diastereomers, in    any mixing ratio, or a corresponding N-oxide thereof, or a    corresponding salt thereof, or a corresponding solvate thereof.

Also preferred are 4-substituted pyrazoline compounds of general formulaI given above, wherein R⁴ represents F; Cl; Br; I; —CN; —NO₂; —NC; —OH;—NH₂; —SH; —C(═O)—H; —C(═O)—OH; —C(═O)—OR¹⁷;

-   a radical selected from the group consisting of methyl, ethyl,    n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl,    n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl,    n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl    and 4-octyl, which may optionally be substituted with 1, 2, 3, 4, 5,    6, 7, 8 or 9 substituent(s) independently selected from the group    consisting of —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃,    —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —CN and —NO₂;-   a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)2—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and    —N(C₂H₅)₂;-   a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclodecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl and diazepanyl, which may optionally    be substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of oxo (═O), thioxo (═S), —CF₃,    methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl,    tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,    —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,    —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃,    —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH,    —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H,    —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,    —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅,    —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃,    —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂;-   a —O—R¹¹ moiety; a —S—R¹² moiety, a —NH—R¹³ moiety or a —NR¹⁴R¹⁵    moiety;-   and X, R¹, R², R³ and R5 to R²² have the meaning given above,    optionally in form of one of the stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of the stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a corresponding salt thereof, or a corresponding solvate    thereof.

Preference is also given to 4-substituted pyrazoline compounds ofgeneral formula I, wherein

-   R⁵ represents H, F; Cl; Br; I; —CN; —NO₂; —NC; —OH; —NH₂; —SH;    —C(═O)—H; —C(═O)—OH; —C(═O)—OR¹⁷;-   a radical selected from the group consisting of methyl, —CF₃, —CH₂F,    —CF₂H, —C₂F₅, ethyl, —CH₂—CN, —CH₂—OH, n-propyl, isopropyl,    —CH₂—CH₂—CN, —CH₂—CH₂—OH, n-butyl, —CH₂—CH₂—CH₂—CN, —CH₂—CH₂—CH₂—OH,    isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl,    neo-pentyl, n-hexyl, 2-hexyl and 3-hexyl;-   a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclodecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl and diazepanyl,-   a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl) and pyrrolyl, which    may be bonded via a —(CH₂)-group and/or may optionally be    substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of —CF₃, methyl, ethyl, n-propyl,    isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,    2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, F, Cl and Br;-   a —O—R¹¹ moiety; a —S—R¹² moiety, a —NH—R¹³ moiety or a —NR¹⁴R¹⁵    moiety;-   and X, R¹ to R⁴ and R ⁶to R²² have the meaning given above,    optionally in form of one of the stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of the stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a corresponding salt thereof, or a corresponding solvate    thereof.

Preference is also given to 4-substituted pyrazoline compounds ofgeneral formula I, wherein

-   R⁴ and R⁵ together with the bridging carbon atom form a radical    selected from the group consisting of cyclopropyl, cyclobutyl,    cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,    cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl,    cyclotetradecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, and    cyclooctenyl, which may optionally be substituted with 1, 2, 3, 4 or    5 substituent(s) independently selected from the group consisting of    oxo (═O), thioxo (═S), —CF₃, methyl, ethyl, n-propyl, isopropyl,    n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,    —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃,    —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,    —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃,    —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,    —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃,    —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,    —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(—O)₂—C₂H₅,    —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂;-   and X, R¹ to R³ and R⁵ to R²² have the meaning given above,    optionally in form of one of the stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of the stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a corresponding salt thereof, or a corresponding solvate    thereof.

Also preferred are 4-substituted pyrazoline compounds of general formulaI given above, wherein R⁶ represents a hydrogen atom; a radical selectedfrom the group consisting of methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl,neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl,4-heptyl, n-octyl, 2-octyl, 3-octyl, 4-octyl vinyl, n-propenyl,n-butenyl, n-pentenyl, n-hexenyl, ethinyl, propinyl, n-butinyl,n-pentinyl and n-hexinyl, which may optionally be substituted with 1, 2,3, 4, 5, 6, 7, 8 or 9 substituent(s) independently selected from thegroup consisting of —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,—O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂, —N(C₂H₅)₂, —CN, —NO, —NH—C(═O)—CH₃, —NH—C(═O)—C₂H₅,—NH—C(—O)—C(CH₃)₃, —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅,—NH—C(═O)—O—C(CH₃)₃, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C(CH₃)₃,—C(—O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —C(═O)—OH, —C(═O)—O—CH₃, —C(—O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅ and —C(—O)—C(CH₃)₃;

-   a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclodecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl, 8-aza-bicyclo[3.2.1]octyl and    diazepanyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,    (CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may optionally be    substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of oxo (═O), thioxo (═S), —CF₃,    methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl,    tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,    —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,    —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃,    —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH,    —SH, —NO₂, —CHO, —C(—O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H,    —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(—O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,    —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅,    —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃,    —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂;-   a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═—O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)2—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,    —N(C₂H₅)₂, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂,    —O—C(═O)—CH₂—CH₂—CH₃, —CH₂—N(CH₃)₂, —(CH₂)—N(C₂H₅)₂, —CH₂—N(C₃H₇)₂,    —CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅) and —(CH₂)-morpholinyl;-   a —P(═O)(OR¹⁶)₂ moiety; a —C(═O)—OR¹⁷ moiety; a —C(═O)—NH—R¹⁸ moiety    or a —C(═O)—R¹⁹ moiety;-   and X, R¹ to R⁵ and R⁷ to R²² have the meaning given above,    optionally in form of one of the stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of the stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a corresponding salt thereof, or a corresponding solvate    thereof.

Preference is also given to 4-substituted pyrazoline compounds ofgeneral formula I given above, wherein R⁷ and R⁸, independently ofanother, in each case represent a hydrogen atom;

-   a radical selected from the group consisting of methyl, ethyl,    n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl,    n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl,    n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl,    4-octyl, 2-(6-methyl)-heptyl, 2-(5-methyl)-heptyl,    2-(5-methyl)-hexyl, 2-(4-methyl)-hexyl, 2-(7-methyl)-octyl;    2-(6-methyl)-octyl, vinyl, n-propenyl, n-butenyl, n-pentenyl,    n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl and n-hexinyl,    which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9    substituent(s) independently selected from the group consisting of    —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,    —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,    —N(C₂H₅)₂, —CN and —NO₂;-   a radical selected from the group consisting of    (1,2,3,4)-tetrahydronaphthyl, (2,3)-dihydro-1H-cyclopenta[b]indolyl,    cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl,    cyclooctyl, cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl,    cyclotridecyl, cyclotetradecyl, cyclopentenyl, cyclohexenyl,    cycloheptenyl, cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl, diazepanyl, azocanyl,    (2,5)-dihydrofuranyl, (2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl,    (2,3)-dihydrofuranyl, (2,5)-dihydro-1H-pyrrolyl,    (2,3)-dihydro-1H-pyrrolyl, tetrahydrothiopyranyl, tetrahydropyranyl,    (3,4)-dihydro-2H-pyranyl, (3,4)-dihydro-2H-thiopyranyl,    (1,2,3,6)-tetrahydropyridinyl, (1,2,3,4)-tetrahydropyridinyl,    (1,2,5,6)-tetrahydropyridinyl, [1,3]-oxazinanyl,    hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl, oxazolidinyl,    (1,3)-dioxanyl, (1,4)-dioxanyl, (1,3)-dioxolanyl, indolinyl,    isoindolinyl, decahydronaphthyl, (1,2,3,4)-tetrahydroquinolinyl,    (1,2,3,4)-tetrahydroisoquinolinyl, octahydro-cyclopenta[c]pyrrolyl,    (1,3,4,7,9a)-hexahydro-2H-quinolizinyl,    (1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,    dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,    (6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,    (2,3)-dihydro-1H-benzo[de]isoquinolinyl,    (1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,    bicyclo[3.1.1]heptyl, norbornenyl, 8-aza-bicyclo[3.2.1]octyl and    8-aza-spiro[4.5]decanyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of oxo (═O), thioxo    (═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,    2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,    —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,    —O—CH₂—O—CH₃, —O—CH₂—CH_(2—O—CH) ₃, —O—CH_(2—O—C) ₂H₅,    —C(OCH₃)(C₂H₅)₂, —C(OCH₃)(CH₃)₂, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃,    —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN,    —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃,    —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,    —C(═O)—O—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃,    —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(—O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,    —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅,    —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂,    —O—Benzyl, benzyl, cyclopentyl, cyclohexyl, pyrrolidinyl and    piperidinyl;-   a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and    —N(C₂H₅)₂;-   a —P(═O)(OR¹⁶)₂ moiety; a —C(═O)—OR¹⁷ moiety; a —C(═O)—NH-R¹⁸    moiety; a —C(═O)—R¹⁹ moiety; a —S(═O)R²⁰ moiety; or a —NR²¹R²²    moiety;-   and X, R¹ to R⁶ and R⁹ to R²² have the meaning given above,    optionally in form of one of the stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of the stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a corresponding salt thereof, or a corresponding solvate    thereof.

Also preferred are 4-substituted pyrazoline compounds of general formulaI given above, wherein R⁹ represents hydrogen or an alkyl radicalselected from the group consisting of methyl, ethyl and n-propyl;

-   and X, R¹ to R⁸ and R¹⁰ to R²² have the meaning given above,    optionally in form of one of the stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of the stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a corresponding salt thereof, or a corresponding solvate    thereof.

Preference is also given to 4-substituted pyrazoline compounds ofgeneral formula I, wherein R¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²⁰,independently of another, in each case represent a radical selected fromthe group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl,isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl,neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl,4-heptyl, n-octyl, 2-octyl, 3-octyl, 4-octyl, 2-(6methyl)-heptyl,2-(5-methyl)-heptyl, 2-(5-methyl)-hexyl, 2-(4-methyl)-hexyl,2-(7-methyl)-octyl; 2-(6methyl)-octyl, vinyl, n-propenyl, n-butenyl,n-pentenyl, n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl andn-hexinyl, which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7,8 or 9 substituent(s) independently selected from the group consistingof —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,—N(C₂H₅)₂, —CN and —NO₂;

-   a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclodecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl, 8-aza-bicyclo[3.2.1]octyl and    diazepanyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,    —(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may optionally be    substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of oxo (═O), thioxo (═S), —CF₃,    methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl,    tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,    —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,    —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃,    —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH,    —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H,    —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,    —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅,    —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃,    —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂;-   or a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH—CH-group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and    —N(C₂H₅)₂;-   and X, R¹ to R⁹, R¹⁶ to R¹⁹, R²¹ and R²² have the meaning given    above, optionally in form of one of the stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of the stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a corresponding salt thereof, or a corresponding solvate    thereof.

Also preferred are 4-substituted pyrazoline compounds of general formulaI given above, wherein R¹⁶, R¹⁷, R¹⁸ and R¹⁹, independently of oneanother, in each case represent a radical selected from the groupconsisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl,n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl,n-octyl, 2-octyl, 3-octyl, 4-octyl, vinyl, n-propenyl, n-butenyl,n-pentenyl, n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl andn-hexinyl, which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7,8 or 9 substituent(s) independently selected from the group consistingof NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH—C(═O)—CH₃,—NH—C(═O)—C₂H₅, —NH—C(═O)—C(CH₃)₃, —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅,—NH—C(═O)—O—C(CH₃)₃, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C(CH₃)₃,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —OH, —C(═O)—OH, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅ and—C(═O)—C(CH₃)₃;

-   or a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)—or —CH═CH—group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)-C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,    —N(C₂H₅)₂, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂,    —O—C(═O)—CH₂—CH₂—CH₃, —CH₂—N(CH₃)₂, —(CH₂)—N(C₂H₅)₂, —CH₂—N(C₃H₇)₂,    —CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅) and —(CH₂)—morpholinyl;-   and X, R¹ to R¹⁵ and R²⁰ to R²² have the meaning given above,    optionally in form of one of the stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of the stereoisomers, preferably enanrtiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a corresponding salt thereof, or a corresponding solvate    thereof.

Also preferred are 4-substituted pyrazoline compounds of general formulaI given above, wherein R²¹ and R²², independently of another, in eachcase represent hydrogen;

-   a radical selected from the group consisting of methyl, ethyl,    n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl,    n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl,    n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl,    4-octyl, 2-(6-methyl)-heptyl, 2-(5-methyl)-heptyl,    2-(5-methyl)-hexyl, 2-(4-methyl)-hexyl, 2-(7-methyl)-octyl;    2-(6-methyl)-octyl, vinyl, n-propenyl, n-butenyl, n-pentenyl,    n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl and n-hexinyl,    which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9    substituent(s) independently selected from the group consisting of    —OH, F, CI, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,    —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,    —N(C₂H₅)₂, —CN and —NO₂;-   a radical selected from the group consisting of    (2,3)-dihydro-1H-cyclopenta[b]indolyl, cyclopropyl, cyclobutyl,    cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,    cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl,    cyclotetradecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl, diazepanyl, azocanyl,    (2,5)-dihydrofuranyl, (2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl,    (2,3)-dihydrofuranyl, (2,5)-dihydro-1H-pyrrolyl,    (2,3)-dihydro-1H-pyrrolyl, tetrahydrothiopyranyl, tetrahydropyranyl,    (3,4)-dihydro-2H-pyranyl, (3,4)-dihydro-2H-thiopyranyl,    (1,2,3,6)-tetrahydropyridinyl, (1,2,3,4)-tetrahydropyridinyl,    (1,2,5,6)-tetrahydropyridinyl, [1,3]-oxazinanyl,    hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl, oxazolidinyl,    (1,3)-dioxanyl, (1,4)-dioxanyl, (1,3)-dioxolanyl, indolinyl,    isoindolinyl, decahydronaphthyl, (1,2,3,4)-tetrahydroquinolinyl,    (1,2,3,4)-tetrahydroisoquinolinyl, octahydro-cyclopenta[c]pyrrolyl,    (1,3,4,7,9a)-hexahydro-2H-quinolizinyl, (1    ,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,    dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,    (6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,    (2,3)-dihydro-1H-benzo[de]isoquinolinyl,    (1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,    bicyclo[3.1.1]heptyl, norbornenyl, 8-aza-bicyclo[3.2.1]octyl and    8-aza-spiro[4.5]decanyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)—or —CH═CH—group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of oxo (═O), thioxo    (═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,    2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,    —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,    —O—CH₂—O—CH₃, —O—CH₂—O—CH₃, —O—CH₂—O—C₂H₅, —C(OCH₃)(C₂H₅)₂,    —C(OCH₃)(CH₃)₂, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,    —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI, B, I, —CN, —OCF₃, —SCF₃,    —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,    —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)    —O—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅,    —C (═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃,    —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇,    —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, cyclopentyl,    cyclohexyl, pyrrolidinyl and piperidinyl;-   or a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)—or —CH═CH-group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and    —N(C₂H₅)₂;-   and X and R¹ to R²⁰ have the meaning given above, optionally in form    of one of the stereoisomers, preferably enantiomers or    diastereomers, a racemate or in form of a mixture of at least two of    the stereoisomers, preferably enantiomers and/or diastereomers, in    any mixing ratio, or a corresponding N-oxide thereof, or a    corresponding salt thereof, or a corresponding solvate thereof.

Also preferred are 4-substituted pyrazoline compounds of general formulaI given above, wherein

-   x is S or O;-   R¹ and R², independently of one another, in each case represent a    radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl, isoindolyl, pyrimidinyl, pyrazinyl, quinolinyl,    isoquinolinyl, benzo[b]yfuranyl, benzo[b]thiophenyl,    benzo[2,1,3]thiadiazolyl, [1,2,31]-benzothiadiazolyl,    [2,1,3]-benzoxadiazolyl, [1,2,3]-benzoxadiazolyl, benzoxazolyl,    benzthiazolyl, benzisoxazolyl, benzisothiazolyl,    imidazo[2,1-b]thiazolyl, 2H-chromenyl, pyranyl, indazolyl,    quinazolinyl, [1,3]-benzodioxolyl, [1 ,4]-benzodioxanyl, [1    ,2,3,4]-tetrahydronaphthyl, (2,3)-dihydro-1H-cyclopenta[b]indolyl,    [1,2,3,4]-tetrahydroquinolinyl, [1,2,3,4]-tetrahydroisoquinolinyl,    [1,2,3,4]-tetrahydroquinazolinyl and    [3,4]-dihydro-2H-benzo[1,4]oxazinyl, which in each case is    optionally bonded to the pyrazoline compound of general formula I    via the aromatic or heteroaromatic part of the aforementioned    radicals and may optionally be substituted with 1, 2, 3, 4 or 5    substituent(s) independently selected from the group consisting of    —CF₃, —CH₂—CI, methyl, ethyl, n-propyl, isopropyl, n-butyl,    isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃,    —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃,    —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,    —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI, Br, I, —CN, —OCF₃, —SCF₃,    —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,    —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH    —C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃,    —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇,    —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂—N(C₂H₅)₂, phenoxy and thiophenyl,    whereby the thiophenyl radical can be substituted with 1, 2 or 3    substituents independently selected from the group consisting of F,    CI, Br, methyl, ethyl and n-propyl;-   or a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl,    cyclotetradecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl, diazepanyl, azocanyl,    (2,5)-dihydrofuranyl, (2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl,    (2,3)-dihydrofuranyl, (2,5)-dihydro-1H-pyrrolyl,    (2,3)-dihydro-1H-pyrrolyl, tetrahydrothiopyranyl, tetrahydropyranyl,    (3,4)-dihydro-2H-pyranyl, (3,4)-dihydro-2H-thiopyranyl,    (1,2,3,6)-tetrahydropyridinyl, (1,2,3,4)-tetrahydropyridinyl,    (1,2,5,6)-tetrahydropyridinyl, [1,3]-oxazinanyl,    hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl, oxazolidinyl,    (1,3)-dioxanyl, (1,4)-dioxanyl, (1,3)-dioxolanyl, indolinyl,    isoindolinyl, decahydronaphthyl, (1,2,3,4)-tetrahydroquinolinyl,    (1,2,3,4)-tetrahydroisoquinolinyl, octahydro-cyclopenta[c]pyrrolyl,    (1 ,3,4,7,9a)-hexahydro-2H-quinolizinyl,    (1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,    dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,    (6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,    (2,3)-dihydro-1H-benzo[de]isoquinolinyl,    (1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1 ]heptyl,    bicyclo[3.1.1 ]heptyl and norbornenyl, which in each case is    optionally bonded to the pyrazoline compound of general formula I    via the (hetero)cycloaliphatic part of the aforementioned radicals    and may optionally be substituted with 1, 2, 3, 4 or 5    substituent(s) independently selected from the group consisting of    oxo (═O), thioxo (═S), —CF₃, methyl, ethyl, n-propyl, isopropyl,    n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,    —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃,    —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,    —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI, Br, I, —CN; —OCF₃, —SCF₃,    —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,    —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃,    —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,    —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅,    —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂;-   R³ represents a radical selected from the group consisting of    (2,3)-dihydro-1H-cyclopenta[b]indolyl, cyclopropyl, cyclobutyl,    cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,    cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl,    cyclotetradecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiornorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl, diazepanyl, azocanyl,    (2,5)-dihydrofuranyl, (2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl,    (2,3)-dihydrofuranyl, (2,5)-dihydro-lH-pyrrolyl,    (2,3)-dihydro-1H-pyrrolyl, tetrahydrothiopyranyl, tetrahydropyranyl,    (3,4)-dihydro-2H-pyranyl, (3,4)-dihydro-2H-thiopyranyl,    (1,2,3,6)-tetrahydropyridinyl, (1,2,3,4)-tetrahydropyridinyl,    (1,2,5,6)-tetrahydropyridinyl, [1,3]-oxazinanyl,    hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl, oxazolidinyl,    (1,3)-dioxanyl, (1,4)-dioxanyl, (1,3)-dioxolanyl, indolinyl,    isoindolinyl, decahydronaphthyl, (1,2,3,4)-tetrahydroquinolinyl,    (1,2,3,4)-tetrahydroisoquinolinyl, octahydro-cyclopenta[c]pyrrolyl,    (1,3,4,7,9a)-hexahydro-2H-quinolizinyl,    (1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,    dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,    (6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,    (2,3)-dihydro-1H-benzo[de]isoquinolinyl,    (1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,    bicyclo[3.1.1]heptyl, norbornenyl, 8-aza-bicyclo[3.2.1]octyl and    8-aza-spiro[4.5]decanyl, which may optionally be substituted with 1,    2, 3, 4 or 5 substituent(s) independently selected from the group    consisting of oxo (═O), thioxo (═S), —CF₃, methyl, ethyl, n-propyl,    isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,    2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,    —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —O—CH₂—O—CH₃, —O—CH₂—CH₂—O—CH₃,    —O—CH₂—O—C₂H₅, —C(OCH₃)(C₂H₅)₂, —C(OCH₃)(CH₃)₂, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO2, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃,    —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,    —N(C₂H₅)₂, —O—Benzyl, benzyl, cyclopentyl, cyclohexyl, pyrrolidinyl    and piperidinyl;-   a —O—R⁶ moiety; a —NR⁷R⁸ moiety or a —NR⁹—O—R¹⁰ moiety;-   R⁴ represents F; CI; Br; I; —CN; —NO₂; —NC; —OH; —NH₂; —SH;    —C(═O)—H; —C(═O)—OH; —C(═O)—OR¹⁷;-   a radical selected from the group consisting of methyl, ethyl,    n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl,    n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl,    n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl    and 4-octyl, which may optionally be substituted with 1, 2, 3, 4, 5,    6, 7, 8 or 9 substituent(s) independently selected from the group    consisting of —OH, F, CI, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃,    —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —CN and —NO₂;-   a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂) —(CH₂)— or —CH═CH—group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH —CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and    —N(C₂H₅)₂;-   a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclodecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl and diazepanyl, which may optionally    be substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of oxo (═O), thioxo (═S), —CF₃,    methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl,    tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,    —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,    —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃,    —S—C(CH₃)₃, F, CI, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH,    —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H,    —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,    —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅,    —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃,    —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂;-   a —O—R¹¹ moiety; a —S—R¹² moiety, a —NH—R¹³ moiety or a —NR¹⁴R¹⁵    moiety;-   R⁴ and R⁵ together with the bridging carbon atom form a radical    selected from the group consisting of cyclopropyl, cyclobutyl,    cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,    cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl,    cyclotetradecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, and    cyclooctenyl, which may optionally be substituted with 1, 2, 3, 4 or    5 substituent(s) independently selected from the group consisting of    oxo (═O), thioxo (═S), —CF₃, methyl, ethyl, n-propyl, isopropyl,    n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,    —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃,    —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,    —S—CH₂—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI, Br, I, —CN, —OCF₃, —SCF₃,    —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,    —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃,    —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,    —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅,    —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂;-   R⁵ represents H, F; CI; Br; I; —CN; —NO₂; —NC; —OH; —NH₂; —SH;    —C(═O)—H; —C(═O)—OH; —C(═O)—OR¹⁷;-   a radical selected from the group consisting of methyl, —CF₃, —CH₂F,    —CF₂H, —C₂F₅, ethyl, —CH₂—CN, —CH₂—OH, n-propyl, isopropyl,    —CH₂—CH₂—CN, —CH₂—CH₂—OH, n-butyl, —CH₂—CH₂—CH₂—CN, —CH₂—CH₂—CH₂—OH,    isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl,    neo-pentyl, n-hexyl, 2-hexyl and 3-hexyl;-   a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclodecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl and diazepanyl;-   a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl) and pyrrolyl, which    may be bonded via a —(CH₂)—group and/or may optionally be    substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of —CF₃, methyl, ethyl, n-propyl,    isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,    2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, F, CI and Br;-   a —O—R¹¹ moiety; a —S—R¹² moiety, a —NH—R¹³ moiety or a —NR¹⁴R¹⁵    moiety;-   R⁶ represents a hydrogen atom; a radical selected from the group    consisting of methyl, ethyl, n-propyl, isopropyl, n-butyi, isobutyl,    sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl,    n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl,    n-octyl, 2-octyl, 3-octyl, 4-octyl vinyl, n-propenyl, n-butenyl,    n-pentenyl, n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl and    n-hexinyl, which may optionally be substituted with 1, 2, 3, 4, 5,    6, 7, 8 or 9 substituent(s) independently selected from the group    consisting of —OH, F, CI, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃,    —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, 13 CN, —NO, —NH—C(═O)—CH₃,    —NH—C(═O)—C₂H₅, —NH—C(═O)—C(CH₃)₃, —NH—C(═O)—O—CH₃,    —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—NH—CH₃,    —C(═O)—NH—C₂H₅, —C(═O)—NH—C(CH₃)₃, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,    —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃,    —C(═O)—CH₃, —C(═O)—C₂H₅ and —C(═O)—C(CH₃)₃;-   a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclodecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl, 8-aza-bicyclo[3.2.1]octyl and    diazepanyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,    —(CH₂)—(CH₂)—(CH₂)— or —CH═CH—group and/or may optionally be    substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of oxo (═O), thioxo (═S), —CF₃,    methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl,    tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,    —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,    —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃,    —S—C(CH₃)₃, F, CI, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH,    —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H,    —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,    —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅,    —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃,    —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂;-   a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, f uryl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH—group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, ——S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,    —N(C₂H₅)₂, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂,    —O—C(═O)—CH₂—CH₂—CH₃, —CH₂—N(CH₃)₂, —(CH₂)—N(C₂H₅)₂, —CH₂—N(C₃H₇)₂,    —CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅) and —(CH₂)—morpholinyl;-   a —P(═O)(OR¹⁶)₂ moiety; a —C(═O)—OR¹⁷ moiety; a —C(═O)—NH—R¹⁸ moiety    or a —C(═O)—R¹⁹ moiety;-   R⁷ and R⁸, independently of another, in each case represent a    hydrogen atom;-   a radical selected from the group consisting of methyl, ethyl,    n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl,    n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl,    n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl,    4-octyl, 2-(6-methyl)-heptyl, 2-(5-methyl)-heptyl,    2-(5-methyl)-hexyl, 2-(4-methyl)-hexyl, 2-(7-methyl)-octyl;    2-(6-methyl)-octyl, vinyl, n-propenyl, n-butenyl, n-pentenyl,    n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl and n-hexinyl,    which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9    substituent(s) independently selected from the group consisting of    —OH, F, CI, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,    —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,    —N(C₂H₅)₂, —CN and —NO₂;-   a radical selected from the group consisting of    (1,2,3,4)-tetrahydronaphthyl, (2,3)-dihydro-1    H-cyclopenta[b]indolyl, cyclopropyl, cyclobutyl, cyclopentyl,    cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, cyclodecyl,    cycloundecyl, cyclododecyl, cyclotridecyl, cyclotetradecyl,    cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl,    pyrrolidinyl, piperidinyl, piperazinyl, homopiperazinyl,    morpholinyl, aziridinyl, azetidinyl, imidazolidinyl,    thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl, diazepanyl, azocanyl,    (2,5)-dihydrofuranyl, (2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl,    (2,3)-dihydrofuranyl, (2,5)-dihydro-1H-pyrrolyl,    (2,3)-dihydro-1H-pyrrolyl, tetrahydrothiopyranyl, tetrahydropyranyl,    (3,4)-dihydro-2H-pyranyl, (3,4)-dihydro-2H-thiopyranyl,    (1,2,3,6)-tetrahydropyridinyl, (1,2,3,4)-tetrahydropyridinyl,    (1,2,5,6)-tetrahydropyridinyl, [1,3]-oxazinanyl,    hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl, oxazolidinyl,    (1,3)-dioxanyl, (1,4)-dioxanyl, (1,3)-dioxolanyl, indolinyl,    isoindolinyl, decahydronaphthyl, (1,2,3,4)-tetrahydroquinolinyl,    (1,2,3,4)-tetrahydroisoquinolinyl, octahydro-cyclopenta[c]pyrrolyl,    (1,3,4,7,9a)-hexahydro-2H-quinolizinyl,    (1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,    dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,    (6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,    (2,3)-dihydro-1H-benzo[de]isoquinolinyl,    (1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,    bicyclo[3.1.1]heptyl, norbornenyl, 8-aza-bicyclo[3.2.1]octyl and    8-aza-spiro[4.5]decanyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH—group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of oxo (═O), thioxo    (═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,    2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,    —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,    —O—CH₂—O—CH₃, —O—CH₂—CH₂—O—CH₃, —O—CH₂—O—C₂H₅, —C(OCH₃)(C₂H₅)₂,    —C(OCH₃)(CH₃)₂, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,    —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI, Br, I, —CN, —OCF₃, —SCF₃,    —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,    —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,    —C(═O)—O—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃,    —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,    —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅,    —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂,    ——O—Benzyl, benzyl, cyclopentyl, cyclohexyl, pyrrolidinyl and    piperidinyl;-   a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH—group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH ₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N (CH₃)₂,    —C(═O)—N(C₂H₅) ₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and    —N(C₂H₅)₂;-   a —P(═O)(OR¹⁶)₂ moiety; a —C(═O)—OR¹⁷ moiety; a —C(═O)—NH—R¹⁸    moiety; a —C(═O)—R¹⁹ moiety; a —S(═O)₂—R²⁰ moiety; or a —NR²R²²    moiety;-   R⁹ represents hydrogen or an alkyl radical selected from the group    consisting of methyl, ethyl and n-propyl;-   R¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²⁰, independently of another, in    each case represent a radical selected from the group consisting of    methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl,    tert-butyl, n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl,    2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl,    2-octyl, 3-octyl, 4-octyl, 2-(6methyl)-heptyl, 2-(5-methyl)-heptyl,    2-(5-methyl)-hexyl, 2-(4-methyl)-hexyl, 2-(7-methyl)-octyl;    2-(6-methyl)-octyl, vinyl, n-propenyl, n-butenyl, n-pentenyl,    n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl and n-hexinyl,    which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9    substituent(s) independently selected from the group consisting of    —OH, F, CI, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,    —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,    —N(C₂H₅)₂, —CN and —NO₂;-   a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclodecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl, 8-aza-bicyclo[3.2.1]octyl and    diazepanyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,    —(CH₂)—(CH₂)—(CH₂)— or —CH═CH—and/or may optionally be substituted    with 1, 2, 3, 4 or 5 substituent(s) independently selected from the    group consisting of oxo (═O), thioxo (═S), —CF₃, methyl, ethyl,    n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and    —N(C₂H₅)₂;-   or a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH—group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl;    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and    —N(C₂H₅)₂;-   R¹⁶, R¹⁷, R¹⁸ and R¹⁹, independently of one another, in each case    represent a radical selected from the group consisting of methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl,    tert-butyl, n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl,    2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl,    2-octyl, 3-octyl, 4-octyl, vinyl, n-propenyl, n-butenyl, n-pentenyl,    n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl and n-hexinyl,    which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9    substituent(s) independently selected from the group consisting of    NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH—C(═O)—CH₃,    —NH—C(═O)—C₂H₅, —NH—C(═O)—C(CH₃)₃, —NH—C(═O)—O—CH₃,    —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—NH—CH₃,    —C(═O)—NH—C₂H₅, —C(═O)—NH—C(CH₃)₃, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,    —OH, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃,    —C(═O)—CH₃, —C(═O)—C₂H₅ and —C(═O)—C(CH₃)₃;-   or a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH—group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, CI,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,    —N(C₂H₅)₂, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂,    —O—C(═O)—CH₂—CH₂—CH₃, —CH₂—N(CH₃)₂, —(CH₂)—N(C₂H₅)₂, —CH ₂—N(C₃H₇)₂,    —CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅) and —(CH₂)—mnorpholinyl; R²¹ and    R²², independently of another, in each case represent hydrogen; a    radical selected from the group consisting of methyl, ethyl,    n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl,    n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl,    n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl,    4-octyl, 2-(6-methyl)-heptyl, 2-(5-methyl)-heptyl,    2-(5-methyl)-hexyl, 2-(4-methyl)-hexyl, 2-(7-methyl)-octyl;    2-(6-methyl)-octyl, vinyl, n-propenyl, n-butenyl, n-pentenyl,    n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl and n-hexinyl,    which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9    substituent(s) independently selected from the group consisting of    —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,    —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,    —N(C₂H₅)₂, —CN and —NO₂;-   a radical selected from the group consisting of    (2,3)-dihydro-1H-cyclopenta[b]indolyl, cyclopropyl, cyclobutyl,    cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,    cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl,    cyclotetradecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl, diazepanyl, azocanyl,    (2,5)-dihydrofuranyl, (2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl,    (2,3)-dihydrofuranyl, (2,5)-dihydro-1H-pyrrolyl,    (2,3)-dihydro-1H-pyrrolyl, tetrahydrothiopyranyl, tetrahydropyranyl,    (3,4)-dihydro-2H-pyranyl, (3,4)-dihydro-2H-thiopyranyl,    (1,2,3,6)-tetrahydropyridinyl, (1,2,3,4)-tetrahydropyridinyl,    (1,2,5,6)-tetrahydropyridinyl, [1,3]-oxazinanyl,    hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl, oxazolidinyl,    (1,3)-dioxanyl, (1,4)-dioxanyl, (1,3)-dioxolanyl, indolinyl,    isoindolinyl, decahydronaphthyl, (1,2,3,4)-tetrahydroquinolinyl,    (1,2,3,4)-tetrahydroisoquinolinyl, octahydro-cyclopenta[c]pyrrolyl,    (1,3,4,7,9a)-hexahydro-2H-quinolizinyl,    (1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,    dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,    (6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,    (2,3)-dihydro-1H-benzo[de]isoquinolinyl,    (1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,    bicyclo[3.1.1]heptyl, norbornenyl, 8-aza-bicyclo[3.2.1]octyl and    8-aza-spiro[4.5]decanyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of oxo (═O), thioxo    (═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,    2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,    —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,    —O—CH₂—O—CH₃, —O—CH₂—CH₂—O—CH₃, —O—CH₂—O—C₂H₅, —C(OCH₃)(C₂H₅)₂,    —C(OCH₃)(CH₃)₂, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,    —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃,    —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,    —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,    —C(═O)—O—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃,    —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,    —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅,    —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂,    cyclopentyl, cyclohexyl, pyrrolidinyl and piperidinyl;-   or a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, is6thiazolyl, imnidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and    —N(C₂H₅)₂;-   optionally in form of one of its stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of its stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a physiologically acceptable salt thereof, or a    corresponding solvate thereof.

Particularly preferred are 4-substituted pyrazoline compounds of generalformula I given above, wherein

-   X is O or S;-   R¹ represents a radical selected from the group consisting of    phenyl, naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl),    pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl, isoindolyl, pyrimidinyl, pyrazinyl, quinolinyl,    isoquinolinyl, benzo[b]furanyl, benzo[b]thiophenyl,    benzo[2,1,3]thiadiazolyl, [1,2,3]-benzothiadiazolyl,    [2,1,3]-benzoxadiazolyl, [1,2,3]-benzoxadiazolyl, benzoxazolyl,    benzthiazolyl, benzisoxazolyl, benzisothiazolyl and    imidazo[2,1-b]thiazolyl, which may optionally be substituted with 1,    2, 3, 4 or 5 substituent(s) independently selected from the group    consisting of —CF₃, —CH₂—Cl, methyl, ethyl, n-propyl, isopropyl,    n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,    —NO₂, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H,    —SCFH₂, phenoxy and thiophenyl, whereby the thiophenyl radical can    be substituted with 1, 2 or 3 substituents independently selected    from the group consisting of F, Cl, Br, methyl, ethyl and n-propyl;-   or a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl and diazepanyl, which may optionally    be substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of —CF₃, methyl, ethyl, n-propyl,    isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,    2-pentyl, n-hexyl, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H and    —SCFH₂;-   R² represents a radical selected from the group consisting of    phenyl, naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl),    pyrrolyl, oxazolyI, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl, isoindolyl, pyrimidinyl, pyrazinyl, quinolinyl,    isoquinolinyl, benzo[b]furanyl, benzo[b]thiophenyl,    benzo[2,1,3]thiadiazolyl, [1,2,3]-benzothiadiazolyl,    [2,1,3]-benzoxadiazolyl, [1,2,3]-benzoxadiazolyl, benzoxazolyl,    benzthiazolyl, benzisoxazolyl, benzisothiazolyl and    imidazo[2,1-b]thiazolyl, which may optionally be substituted with 1,    2, 3, 4 or 5 substituent(s) independently selected from the group    consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,    isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —OH,    —O—CH₃, —O—C₂H₅, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H and —SCFH₂;-   or a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, 10 cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl and diazepanyl, which may, optionally    be substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of —CF₃, methyl, ethyl, n-propyl,    isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,    2-pentyl, n-hexyl, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H and    —SCFH₂;-   R³ represents a radical selected from the group consisting of    which is in each case bonded to the pyrazoline compound of general    formula I in any position of the cyclic part of the aforementioned    radicals including the NH-groups, preferably said radicals are    bonded to the pyrazoline compound of general formula I at the    nitrogen atom of the cyclic part of the aforementioned radicals;-   a —O—R⁶ moiety, a —NR⁷R⁸ moiety or a —NR⁹—O—R¹⁰ moiety;-   R⁴ represents F; Cl; Br; I; —CN; —NO₂; —NC; —OH; —NH₂; —SH;    —C(═O)—H; —C(═O)—OH; —C(═O)—OR¹⁷;-   a radical selected from the group consisting of methyl, —CF₃, —CH₂F,    —CF₂H, —C₂F₅, ethyl, —CH₂—CN, —CH₂—OH, n-propyl, isopropyl,    —CH₂—CH₂—CN, —CH₂—CH₂—OH, n-butyl, —CH₂—CH₂—CH₂—CN, —CH₂—CH₂—CH₂—OH,    isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl,    neo-pentyl, n-hexyl, 2-hexyl and 3-hexyl;-   a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl) and pyrrolyl, which    may be bonded via a —(CH₂)— group and/or may optionally be    substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of —CF₃, methyl, ethyl, n-propyl,    isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,    2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, F, Cl and Br; a —O—R¹¹ moiety; a    —S—R¹² moiety, a —NH—R¹³ moiety or a —NR¹⁴R¹⁵ moiety;-   R⁵ represents H; F; Cl; Br; —C(═O)—OH; —C(═O)—OR¹⁷; or an alkyl    radical selected from the group consisting of methyl, ethyl,    n-propyl, isopropyl and n-butyl;-   or R⁴ and R⁵ together with the bridging carbon atom form a radical    selected from the group consisting of cyclopropyl, cyclobutyl,    cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclopentenyl,    cyclohexenyl, cycloheptenyl and cyclooctenyl;-   R⁶ represents a hydrogen atom; a radical selected from the group    consisting of methyl, —CF₃, —CH₂F, —CF₂H, —CH₂—O—CH₃, —C₂F₅,    —CH₂—CH₂—F, ethyl, —CH₂—CN, —CH₂—OH, n-propyl, isopropyl,    —CH₂—CH₂—CN, —CH₂—CH₂—OH, —CH₂—CH₂—OCH₃, n-butyl, —CH₂—CH₂—CH₂—CN,    —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—O—CH₃, isobutyl, sec-butyl,    -tert-butyl, n-pentyl, —CH₂—CH₂—CH₂—CH₂—O—CH₃, 2-pentyl, 3-pentyl,    neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl and n-octyl;-   a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, pyrrolidinyl,    piperidinyl, piperazinyl, homopiperazinyl, morpholinyl,    imidazolidinyl, azepanyl, 8-aza-bicyclo[3.2.1]octyl and diazepanyl,    which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,    —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or may optionally be    substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of oxo (═O), thioxo (═S), methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃ and —O—C(CH₃)₃;-   a radical selected from the group consisting of pyridinyl, furyl    (furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl,    thiazolyl, isothiazolyl and imidazolyl, which may be bonded via a    —(CH₂)—, —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or    may optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of methyl, ethyl,    n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, F, Cl, Br, I,    —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂,    —O—C(═O)—CH₂—CH₂—CH₃, —CH₂—N(CH₃)₂, —(CH₂)—N(C₂H₅)₂, —CH₂—N(C₃H₇)₂,    —CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅) and —(CH₂)-morpholinyl; a    —P(═O)(OR¹⁶)₂ moiety; a —C(═O)—OR¹⁷ moiety; a —C(═O)—NH—R¹⁸ moiety    or a —C(═O)—R¹⁹ moiety.-   R⁷ and R⁸, independently of another, in each case represent a    hydrogen atom;-   a radical selected from the group consisting of methyl, ethyl,    n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl,    n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl,    n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl,- n-octyl, 2-octyl, 3-octyl,    4-octyl, 2-(6-methyl)-heptyl, 2-(5-methyl)-heptyl,    2-(5-methyl)-hexyl, 2-(4-methyl)-hexyl, 2-(7-methyl)-octyl;    2-(6-methyl)-octyl, —CH₂—NH₂, —CH₂—N(CH₃)₂, —CH₂—CH—NH₂,    —CH₂—CH₂—N(CH₃)₂, —CH₂—CH₂—N(C₂H₅)₂, —CH₂—CH₂—CH₂—NH₂,    —CH₂—CH₂—CH₂—N(CH₃)₂ and —CH₂—CH₂—CH₂—N(C₂H₅)₂;-   a radical selected from the group consisting of morpholinyl,    piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, cyclopentyl,    cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, cyclodecyl,    cycloundecyl, cyclododecyl, cyclotridecyl, cyclotetradecyl,    [1,2,3,4]-tetrahydronaphthyl and bicyclo[2.2.1]heptyl, which may be    bonded via a —(CH₂)—, —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH—    group and/or may optionally be substituted with 1, 2, 3, 4 or 5    substituent(s) independently selected from the group consisting of    —OH, —O—CH₃, —O—C₂H₅, —O-Benzyl, benzyl, methyl, ethyl, n-propyl,    isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,    2-pentyl and n-hexyl;-   a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl) and triazolyl,    which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,    —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or may optionally be    substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of —CF₃, methyl, ethyl, n-propyl,    isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,    2-pentyl, n-hexyl, F, Cl and Br;-   a —S(═O)₂—R²⁰ moiety;-   a —NR²¹R²² moiety;-   a radical selected from the group consisting of    which is in each case bonded to the pyrazoline compound of general    formula I in any position of the cyclic part of the aforementioned    radicals including the NH— groups, optionally via a —(CH₂)— or    —(CH₂)—(CH₂)— group, preferably said radicals are bonded to the    pyrazoline compound of general formula I at the nitrogen atom of the    cyclic part of the aforementioned radicals;-   R⁹ represents hydrogen;-   R¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²⁰ independently of another, in    each case represent a radical selected from the group consisting of    methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl,    tert-butyl, n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl,    2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl,    2-octyl, 3-octyl, 4-octyl, 2-(6methyl)-heptyl, 2-(5-methyl)-heptyl,    2-(5-methyl)-hexyl, 2-(4-methyl)-hexyl, 2-(7-methyl)-octyl;    2-(6-methyl)-octyl, vinyl, n-propenyl, n-butenyl, n-pentenyl,    n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl and n-hexinyl,    which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9    substituent(s) independently selected from the group consisting of    —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,    —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,    —N(C₂H₅)₂, —CN and —NO₂;-   a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclodecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,    cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,    homopiperazinyl, morpholinyl, aziridinyl, azetidinyl,    imidazolidinyl, thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl,    tetrahydrothiophenyl, azepanyl, 8-aza-bicyclo[3.2.1]octyl and    diazepanyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,    —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or may optionally be    substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of oxo (═O), thioxo (═S), —CF₃,    methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl,    tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,    —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,    —S—C₂H₅, —S—CH₂CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃,    F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂,    —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂,    —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,    —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅,    —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃,    —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂;-   or a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and    —N(C₂H₅)₂;-   R¹⁶, R¹⁷, R¹⁸ and R¹⁹, independently of one another, in each case    represent a radical selected from the group consisting of methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl,    tert-butyl, n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl,    2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl,    2-octyl, 3-octyl, 4-octyl, vinyl, n-propenyl, n-butenyl, n-pentenyl,    n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl and n-hexinyl,    which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9    substituent(s) independently selected from the group consisting of    NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH—C(═O)—CH₃,    —NH—C(═O)—C₂H₅, —NH—C(═O)—C(CH₃)₃, —NH—C(═O)—O—CH₃,    —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—NH—CH₃,    —C(═O)—NH—C₂H₅, —C(═O)—NH—C(CH₃)₃, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,    —OH, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃,    —C(═O)—CH₃, —C(═O)—C₂H₅ and —C(═O)—C(CH₃)₃;-   or a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,    oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,    pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl,    indolyl and isoindolyl, which may be bonded via a —(CH₂)—,    —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or may    optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —CF₃, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃,    —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,    —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl,    Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,    —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,    —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,    —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,    —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,    —N(C₂H₅)₂, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂,    —O—C(═O)—CH₂—CH₂—CH₃, —CH₂—N(CH₃)₂, —(CH₂)—N(C₂H₅)₂, —CH₂—N(C₃H₇)₂,    —CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅) and —(CH₂)-morpholinyl;    and-   R²¹ and R²², independently of another, in each case represent    hydrogen;-   a radical selected from the group consisting of methyl, ethyl,    n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl,    n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl,    n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl,    4-octyl, 2-(6-methyl)-heptyl, 2-(5-methyl)-heptyl,    2-(5-methyl)-hexyl, 2-(4-methyl)-hexyl, 2-(7-methyl)-octyl;    2-(6-methyl)-octyl, —CH₂—NH₂, —CH—N(CH₃)₂, —CH₂—CH—NH₂,    —CH₂—CH₂—N(CH₃)₂, —CH₂—CH₂—N(C₂H₅)₂, —CH₂—CH₂—CH₂—NH₂,    —CH₂—CH₂—CH₂—N(CH₃)₂ and —CH₂—CH₂—CH₂—N(C₂H₅)₂;-   a radical selected from the group consisting of cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl,    cyclotetradecyl and bicyclo[2.2.1]heptyl, which may be bonded via a    —(CH₂)—, —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or    may optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)    independently selected from the group consisting of —OH, methyl,    ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl,    n-pentyl, 2-pentyl and n-hexyl;-   a radical selected from the group consisting of phenyl, naphthyl,    pyridinyl, furyl (furanyl), thienyl (thiophenyl) and triazolyl,    which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,    —(CH₂)—(CH₂)—(CH₂)— or ——CH═CH—group and/or may optionally be    substituted with 1, 2, 3, 4 or 5 substituent(s) independently    selected from the group consisting of —CF₃, methyl, ethyl, n-propyl,    isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,    2-pentyl, n-hexyl, F, Cl and Br;-   or a radical selected from the group consisting of    which is in each case bonded to the pyrazoline compound of general    formula I in any position of the cyclic part of the aforementioned    radicals including the NH-groups, preferably said radicals are    bonded to the pyrazoline compound of general formula I at the    nitrogen atom of the cyclic part of the aforementioned radicals;-   optionally in form of one of its stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of its stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a physiologically acceptable salt thereof, or a    corresponding solvate thereof.

More particularly preferred are 4-substituted pyrazoline compounds ofgeneral formula I given above, wherein

-   X is O or S;-   R¹ represents a radical selected from the group consisting of phenyl    and thienyl (thiophenyl), which may optionally be substituted with    1, 2, 3, 4 or 5 substituent(s) independently selected from the group    consisting of —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br and I;-   R² represents a phenyl radical, which may be substituted with 1, 2,    3, 4 or 5 substituent(s) independently selected from the group    consisting of —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br and I;-   R³ represents a radical selected from the group consisting of    which is in each case bonded to the pyrazoline compound of general    formula I in any position of the cyclic part of the aforementioned    radicals including the NH— groups, preferably said radicals are    bonded to the pyrazoline compound of general formula I at the    nitrogen atom of the cyclic part of the aforementioned radicals;-   a —OR⁶-moiety or a —NR⁷R⁸ moiety;-   R⁴ represents F; Cl; Br; I; —OH, —CN; —C(═O)—H; —C(═O)—OH;    —C(═O)—OR¹⁷;-   a radical selected from the group consisting of methyl, —CF₃, —CH₂F,    —CF₂H, —C₂F₅, ethyl, —CH₂—CN, —CH₂—OH, n-propyl, isopropyl,    —CH₂—CH₂—CN, —CH₂—CH₂—OH, n-butyl, —CH₂—CH₂—CH₂—CN, —CH₂—CH₂—CH₂—OH,    isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl,    neo-pentyl, n-hexyl, 2-hexyl and 3-hexyl;-   a benzyl radical or a —O—R¹¹ moiety;-   R⁵ represents H; F; Cl; Br; —C(═O)—OH; —C(═O)—OR¹⁷; or a radical    selected from the group consisting of methyl, ethyl, n-propyl,    isopropyl and n-butyl;-   or R⁴ and R⁵ together with the bridging carbon atom form a radical    selected from the group consisting of cyclopropyl, cyclobutyl,    cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclopentenyl,    cyclohexenyl, cycloheptenyl and cyclooctenyl;-   R⁶ represents a hydrogen atom; a radical selected from the group    consisting of methyl,) ethyl, n-propyl, isopropyl, n-butyl and    tert-butyl or a radical selected from the group consisting of    cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl;-   R⁷ represents a hydrogen atom or a radical selected from the group    consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl    and tert-butyl;-   R⁸ represents a radical selected from the group consisting of    [1,2,3,4]-tetrahydronaphthyl, bicyclo[2.2.1]heptyl, cyclopropyl,    cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,    cyclononyl, cyclodecyl, cycloundecyl and cyclododecyl, which may be    bonded via a —(CH₂)—, —(CH₂)—(CH₂)— or —(CH₂)—(CH₂)—(CH₂)— group    and/or substituted with 1, 2, 3 or 4 substituents selected from the    group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl,    sec-butyl, tert-butyl, —OH, —O—CH₃ and —O—C₂H₅;-   or a radical selected from the group consisting of    which is in each case bonded to the pyrazoline compound of general    formula I in any position of the cyclic part of the aforementioned    radicals including the NH— groups, preferably said radicals are    bonded to the pyrazoline compound of general formula I at the    nitrogen atom of the cyclic part of the aforementioned radicals;    and-   R¹¹ and R¹⁷, independently of one another, each represent a radical    selected from the group consisting of methyl, ethyl, n-propyl,    isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl,    2-pentyl, 3-pentyl and neo-pentyl;-   optionally in form of one of its stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of its stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a physiologically acceptable salt thereof, or a    corresponding solvate thereof.

Also more particularly preferred are 4-substituted pyrazoline compoundsof general formulae L, M or N,

wherein

-   R^(L) represents —OH or oxo (═O);-   X is O or S;-   R¹ represents a radical selected from the group consisting of phenyl    and thienyl (thiophenyl), which may optionally be substituted with 1    substituent selected from the group consisting of —OH, —O—CH₃,    —O—C₂H₅, F, Cl, Br and I;-   R² represents a phenyl radical, which may be substituted with 1 or 2    substituent(s) independently selected from the group consisting of    —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br and I;-   R⁴ represents F; Cl; Br; I; —OH, —CN; —C(═O)—H; —C(═O)—OH;    —C(═O)—OR¹⁷;-   a radical selected from the group consisting of methyl, —CF₃, —CH₂F,    —CF₂H, —C₂F₅, ethyl, —CH₂—CN, —CH₂—OH, n-propyl, isopropyl,    —CH₂—CH₂—CN, —CH₂—CH₂—OH, n-butyl, —CH₂—CH₂—CH₂—CN, —CH₂—CH₂—CH₂—OH,    isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl,    neo-pentyl, n-hexyl, 2-hexyl and 3-hexyl,-   a benzyl radical or a —O—R¹¹ moiety;-   R⁵ represents H; F; Cl; Br; —C(═O)—OH; —C(═O)—OR¹⁷; or radical    selected from the group consisting of methyl, ethyl, n-propyl,    iso-propyl and n-butyl;-   or R⁴ and R⁵ together with the bridging carbon atom form a radical    selected from the group consisting of cyclopropyl, cyclobutyl,    cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclopentenyl,    cyclohexenyl, cycloheptenyl and cyclooctenyl;    and-   R¹¹ and R¹⁷, independently of one another, each represent a radical    selected from the group consisting of methyl, ethyl, n-propyl,    isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl,    2-pentyl, 3-pentyl, and neo-pentyl;-   optionally in form of one of its stereoisomers, preferable    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of its stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a physiologically acceptable salt thereof, or a    corresponding solvate thereof.

Also more particularly preferred are 4-substituted pyrazoline compoundof general formulae L, M or N,

wherein

-   R^(L) represents H, —OH or oxo (═O);-   X is O or S;-   R² represents a phenyl radical, which may be substituted with 1 or 2    substituent(s) independently selected from the group consisting of    —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br and I;-   R⁴ represents F; Cl; Br; I; —OH, —CN; —C(═O)—H; —C(═O)—OH;    —C(═O)—OR¹⁷;-   a radical selected from the group consisting of methyl, —CF₃, —CH₂F,    —CF₂H, —C₂F₅, ethyl, —CH₂—CN, —CH₂—OH, n-propyl, isopropyl,    —CH₂—CH₂—CN, —CH₂—CH₂—OH, n-butyl, —CH₂—CH₂—CH₂—CN, —CH₂—CH₂—CH₂—OH,    isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl,    neo-pentyl, n-hexyl, 2-hexyl and 3-hexyl;-   a benzyl radical or a O—R¹¹ moiety;-   R⁵ represents H; F; Cl; Br; —C(═O)—OH; —C(═O)—OR¹⁷; or a radical    selected from the group consisting of methyl, ethyl, n-propyl,    iso-propyl and n-butyl;-   or R⁴ and R⁵ together with the bridging carbon atom form a radical    selected from the group consisting of cyclopropyl, cyclobutyl,    cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclopentenyl,    cyclohexenyl, cycloheptenyl and cyclooctenyl;    and-   R¹¹ and R¹⁷, independently of one another, each represent a radical    selected from the group consisting of methyl, ethyl, n-propyl,    isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl,    2-pentyl, 3-pentyl and neo-pentyl;-   optionally in form of one of its stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of its stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a physiologically acceptable salt thereof, or a    corresponding solvate thereof.

Most particularly preferred are 4-substituted pyrazoline compounds ofgeneral formula I given above selected from the group consisting of

-   [1]    cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamride hydro-chloride-   [2]    trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide hydro-chloride-   [3]    cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid azepan-1-ylamide-   [4]    trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid azepan-1-ylamide-   [5]    cis-[5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-(4-cyclohexyl-piperazin-1-yl)-methanone-   [6]    trans-[5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-(4-cyclohexyl-piperazin-1-yl)-methanone-   [7]    cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid pyrrolidin-1-ylamide-   [8]    trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid pyrrolidin-1-ylamide-   [9]    cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid (4-methyl-piperidin-1-yl)-amide-   [10]    trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid (4-methyl-piperidin-1-yl)-amide-   [11]    cis-[5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-piperidin-1-yl-methanone-   [12]    trans-[5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-piperidin-1-yl-methanone-   [13]    cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid (hexahydro-cyclopenta[c]pyrrol-2-yl)-amide-   [14]    trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid (hexahydro-cyclopenta-[c]py-rrol-2-yl)-amide-   [15]    cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid (2,3-dihydro-indol-1-yl)-amide-   [16]    trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid (2,3-dihydro-indol-1-yl)-amide-   [17]    cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid cyclobutylamide-   [18]    5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid cyclo-hexyl methyl-amide-   [19]    cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   [20]    trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-py-razole-3-carboxylic    acid-   [21]    cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   [22]    trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [23]    cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid methyl ester-   [24]    trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid methyl ester-   [25]    cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid ethyl ester-   [26]    trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro1H-py-razole-3-carboxylic    acid ethyl ester-   [27]    5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid cyclohexyl ester-   [28]    5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4,4-dimethyl-4,5-dihydro-1-H-pyrazole-3-carboxylic    acid-   [29]    5-(4-Chloro-phenyl)-1-(2,4-dichlorophenyl)-4,4-dimethyl-4,5-dihydro-1-H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [30]    5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [31]    5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   [32]    5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [33]    5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-(2-hydroxy-ethyl)-4,5-di-hydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [34]    5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-(2-hydroxy-ethyl)-4,5-di-hydro-1H-pyrazole-3-carboxylic    acid-   [35]    5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazol-3-carboxylic    acid piperidin-1-ylamide-   [36]    5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazol-3carboxylic    acid-   [37]    5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [38]    5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   [39]    5-(4-chlorophenyl)-4-cyano-1-(2,4-dichlorophenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   [40]    5-(4-Chloro-phenyl)-4-cyano-1-(2,4-dichloro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   [41]    1-(2,4-Dichloro-phenyl)-5-(4-fluoro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [42]    1-(2,4-Dichloro-phenyl)-4-ethyl-5-(4-fluoro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [43]    1-(2,4-Dichloro-phenyl)-5-(4-fluoro-phenyl)-4,4-dimethyl-4,5-dihydro-1-H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [44]    1-(2,4-Dichloro-phenyl)-5-(4-fluoro-phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [45]    1-(2,4-Dichloro-phenyl)-5-(4-fluoro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [46]    1-(2,4-Dichloro-phenyl)-5-(4fluoro-phenyl)-4-(2-hydroxy-ethyl)-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [47]    1-(2,4-Dichloro-phenyl)-4-fluoromethyl-5-(4-fluoro-phenyl)-4,5-dihydro-1H-pyrazol-3-carboxylic    acid piperidin-1-ylamide-   [48]    1-(2,4-Dichloro-phenyl)-5-(4fluoro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [49]    4-Cyano-1-(2,4-dichloro-phenyl)-5-(4-fluoro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [50]    5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [51]    5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [52]    5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [53]    5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [54]    5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [55]    5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-(2-hydroxy-ethyl)-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [56]    5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [57]    5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [58]    5-(4-Bromo-phenyl)-4-cyano-1-(2,4-dichloro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [59]    cis-5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [60]    trans-5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [61]    cis-5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [62]    trans-5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [63]    5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [64]    5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [65]    5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [66]    5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-(2-hydroxy-ethyl)-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [67]    5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [68]    5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [69]    5-(5-Chloro-thiophen-2-yl)-4-cyano-1-(2,4-dichloro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide [70]    cis-5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [71]    trans-5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [72]    cis-5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [73]    trans-5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [74]    5-(5-Bromo-thiophen-2-yl)-1-(2,4-di-chlorophenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [75]    cis-5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [76]    trans-5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [77]    cis-5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [78]    trans-5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [79]    5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [80]    5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [81]    5-(5-Bromo-thiophen-2-yl)-1-(2,4-di-chloro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [82]    5-(5-Bromo-thiophen-2-yl)-1-(2,4-di-chloro-phenyl)-4-(2-hydroxy-ethyl)-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [83]    5-(5-Bromo-thiophen-2-yl)-1-(2,4-di-chloro-phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [84]    5-(5-Bromo-thiophen-2-yl)-1-(2,4-di-chloro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [85]    5-(5-Bromo-thiophen-2-yl)-4-cyano-1-(2,4-dichloro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   [86]    cis-5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   [87]    trans-[5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-piperidin-1-yl-methanone-   [88]    cis-5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   [89]    trans-5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   [90]    cis-5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   [91]    trans-5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid,-   92    (+)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   93    (−)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   94    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   95    trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   96    cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid azepan-1-ylamide hydrochloride-   97    trans-5-(4-Chlorophenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid azepan-1-ylamide hydrochloride-   98    cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   99    trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   100    cis-5-(4-chlorophenyl)-N-(4-cyclopentylpiperazin-1-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   101    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-morpholino-4,5-dihydro-1H-pyrazole-3-carboxamide-   102    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(4-methylpiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   103    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(2,6-dimethylpiperidin-1-yl)-4-methyl-4,5-dihydro6-1H-pyrazole-3-carboxamide-   104    cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid (1,3-dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-amide-   105    cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid (1H,3H-benzo[de]isoquinolin-2-yl)-amide-   106    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((R)-2-(methoxymethyl)pyrrolidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   107    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((S)-2-(methoxymethyl)pyrrolidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   108    cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid (hexahydro-cyclopenta[c]pyrrol-2-yl)-amide hydrochloride-   109    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   110    trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   111    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   112    trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   113    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(2-methylindolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   114    cis-5-(4-chlorophenyl)-N-(cyclohexylmethyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   115    cis-5-(4-chlorophenyl)-N-(cycloheptylmethyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   116    cis-5-(4-chlorophenyl)-N-cyclododecyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   117    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   118    cis-N-(4-tert-butylcyclohexyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   119    cis-5-(4-chlorophenyl)-N-cyclooctyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   120    cis-N-(azocan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   121    cis-N-(azocan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   122    cis-azocan-1-yl(cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl)methanone-   123    cis-5-(4-chlorophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   124    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-cycloheptyl-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   125    trans-5-(4-chlorophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   126    trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-cycloheptyl-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   127    cis-5-(4-chlorophenyl)-N-(cyclohexylmethyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   128    (+)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   129    (−)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   130    (−)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1R,2R)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   131    (+)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1R,2R)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   132    (+)-cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   133    (−)-cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   134    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(4-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   135    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(4-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   136    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(3-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   137    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(3-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   138    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(2-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   139    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(2-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   140    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(4-oxopiperidin-1-yl)-4,5dihydro-1H-pyrazole-3-carboxamide-   141    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(4-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   142    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(3-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   143    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4methyl-N-(3-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   144    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(3,4-dihydropyridin-1(2H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   145    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(3,4-dihydropyridin-1(2H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   146    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(5,6-dihydropyridin-1(2H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   147    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(5,6-dihydropyridin-1(2H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   148    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   149    trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   150    cis-5-(4-Chlorophenyl)-1-(2,4-dichiorophenyl)-4-methyl-4,5-dihydro-1H-py-razole-3-carboxylic    acid cyclohexyl ester-   151    N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   152    1-(2-chlorophenyl)-5-(4-chlorophenyl)-4,4-dimethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   153    N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   154    cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   155    trans-5-(4-Chloro-phenyl)-1-(2,4-dichlorophenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid piperidin-1-ylamide-   156    cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   157    trans-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   158    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   159 trans    1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   160    5-(4-chlorophenyl)-1-(2j4-dichlorophenyl)-3-(piperidin-1-ylcarbamoyl)-4,5-dihydro-1H-pyrazole-4-carboxylic    acid-   161    5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,4-difluoro-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   162    cis-5-(4chlorophenyl)-4-cyano-1-(2,4-dichlorophenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   163    cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-4-cyano-1-(2,4dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   164cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-cyano-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   165    cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-cyano-4,5-dihydro-1H-pyrazole-3-carboxamide-   166    trans-5-(4-chlorophenyl)-4-cyano-1-(2,4-dichlorophenyI)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   167    trans-N-(azepan-1-yl)-5-(4-chlorophenyl)-4-cyano-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   168    trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-cyano-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   169    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   170    trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   171    cis5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   172    trans-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   173cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   174    trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   175 cis    -N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   176    trans-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   177    cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   178    trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   179    cis-5-(4-chlorophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   180    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-cycloheptyl-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   181    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   182    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   183    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(indolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   184    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-N-(indolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   185    cis5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   186    trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   187    cis5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   188    trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   189    cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   190    trans-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   191    cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   192    cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   193    cis5-(4-bromophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   194    cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-cycloheptyl-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   195    cis5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   196    cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   197cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(indolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   198    cis5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-N-(indolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   199    cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   200    trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   201    cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   202    trans-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   203    cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   204    trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   205    cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1pyrazole-3-carboxamide-   206    trans-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   207    cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   208    trans-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   209    cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   210    cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   211    cis-5-(4-bromophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   212    cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-cycloheptyl-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   213    cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   214    cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   215    cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   216    cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   217    (+)-cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   218    (−)-cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   219    (+)-cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   220    (−)-cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   221    cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   222trans-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   223    cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   224    trans-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    225    cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   226    trans-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   227    cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   228    trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-4fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   229    cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   230    trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   231    cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   232    cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   233    cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   234    cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   235    cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   236    cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   237    (+)-cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   238    (−)-cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   239    (+)-cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   240    (−)-cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   241    cis-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   242    trans-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   243    cis-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   244    trans-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   245    cis-1-(2-chlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   246    trans-1-(2-chlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   247    cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   248    trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   249    cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   250    trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-iodophenyl)-4methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   251    cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   252    cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   253    cis-1-(2,4-dichlbrophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   254    cis-1-(2-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   255    cis-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   256    cis-1-(2-chlorophenyl)-N-(indolin-1-yl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   257    (+)-cis-1-(2,4-dichlorophenyl)-N-((1$,2S)-2-hydroxycyclohexyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   258    (−)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   259    (+)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   260    (−)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   261    cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   262    trans-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   263    cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   264    trans-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   265    cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   266    (+)-cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   267    (−)-cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   268    trans-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   269    cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   270    trans-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   271    cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   272    trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   273    cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   274    trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   275    cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   276    cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-methoxyphenyl)--methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   277    cis-1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   278    cis-1-(2-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   279    cis-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   280    cis-1-(2-chlorophenyl)-N-(indolin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   281    (+)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   282    (−)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   283    (+)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   284    (−)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   285    cis-1-(2,4-dichlorophenyl)-N-(4-hydroxypiperidin-1-yl)-5-(4methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    286    cis-1-(2-chlorophenyl)-N-(4-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   287    cis-1-(2,4-dichlorophenyl)-N-(3-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   288    cis-1-(2-chlorophenyl)-N-(3-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   289    cis-1-(2,4-dichlorophenyl)-N-(2-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   290    cis-1-(2-chlorophenyl)-N-(2-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   291    cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(4-oxopiperidin-1yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   292    cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(4-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   293    cis-1-(2,4-dichlorophenyl)-5-(4methoxyphenyl)-4-methyl-N-(3-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   294    cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(3-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   295    cis-1-(2,4-dichlorophenyl)-N-(3,4dihydropyridin-1(2H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   296    cis-1-(2-chlorophenyl)-N-(3,4-dihydropyridin-1(2H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   297    cis-1-(2,4-dichlorophenyl)-N-(5,6-dihydropyridin-1(2H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   298    cis-1-(2-chlorophenyl)-N-(5,6-dihydropyridin-1(2H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   299    cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   300    trans-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   301    cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   302    trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   303    cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   304    trans-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   305    1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4,4-dimethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   306    N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   307    1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4,4-dimethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   308    1-(2,4-dichlorophenyl)-4-formyl-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   309    1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-3-(piperidin-1-ylcarbamoyl)-4,5-dihydro-1H-pyrazole-4-carboxylic    acid-   310    1-(2,4-dichlorophenyl)-4-(2-hydroxyethyl)-5-(4methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   311    1-(2,4-dichlorophenyl)-4-(fluoromethyl)-5-(4methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   312    cis-4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   313    trans-4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   314    cis-N-(azepan-1-yl)-4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   315    trans-N-(azepan-1-yl)-4cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   316 cis    -1-(2-chlorophenyl)-4-cyano-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   317    trans-1-(2-chlorophenyl)-4-cyano-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   318    1-(2,4-dichlorophenyl)-4-hydroxy-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   319    1-(2-chlorophenyl)-4,4-difluoro-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   320    1-(2-chlorophenyl)-4-formyl-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   321    1-(2-chlorophenyl)-5-(4-methoxyphenyl)-3-(piperidin-1-ylcarbamoyl)-4,5-dihydro-1H-pyrazole-4-carboxylic    acid-   322    1-(2-chlorophenyl)-4-(2-hydroxyethyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   323    1-(2-chlorophenyl)-4-(fluoromethyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   324    1-(2-chlorophenyl)-4-hydroxy-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   325    cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   326    trans-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   327    cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   328    trans-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   329    cis-N-(azepan-1-y)-1-(2,4-dichlorophenyl)-5-(4ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   330    trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   331 cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)    4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   332    trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   333    cis-N-cycloheptyl-1-(2,4dichlorophenyl)-5-(4-ethoxyphenyl)-4-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   334    cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   335    cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   336    cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   337    cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-1H-pyrazole-3-carboxamide-   338    cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   339    (+)-cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-N-((1,S2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   340    (−)-cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-N-((1,S2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   341    (+)-cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   342    (−)-cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   343    cis-1-(2,4-dichlorophehyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   344    trans-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   345    cis-1-(2chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   346    trans-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   347    cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   348    trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   349    cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   350    trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   351    cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro1H-pyrazole-3-carboxamide-   352    cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   353    cis-1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   354    cis-1-(2-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   355    cis-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   356    cis-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   357    (+)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   358    (−)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   359    (+)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   360    (−)-cis-)-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   361    cis-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   362    trans-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   363    cis-1-(2-chlorophenyl)-5-(5-chlorothiophen-2-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   364    trans-1-(2-chlorophenyl)-5-(5-chlorothiophen-2-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   365    cis-5-(5-bromothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   366    trans-5-(5-bromothiophen-2-yl)-1-(2,4dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   367    cis-1-(2,4-dichlorophenyl)-4-methyl-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   368    trans-1-(2,4-dichlorophenyl)-4-methyl-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   369    cis-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   370    trans-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   371    cis-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1-pyrazole-3-carboxamide-   372    trans-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   373    cis-1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   374    trans-1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   375    cis-1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   376    trans-1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   377    cis-1-(2-chlorophenyl)-4-methyl-5-phenyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   378    trans-1-(2-chlorophenyl)-4methyl-5-phenyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   379    cis-5-(4-chlorophenyl)-1-(2,4dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide    hydrochloride-   380    trans-5-(4-chlorophenyl)-1-(2,4-dichlorophehyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   381    cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   382    trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   383    cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbothioamide-   384    cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbothioamide-   385    cis-5-(4-bromophenyl)-1-(2,4dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   386    trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide

387cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide

-   388    trans-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   389    cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   390    trans-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   391    cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   392    trans-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   393    cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   394    cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbothioamide-   395    trans-1-(2,4dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   396    cis1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   397    cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbothioamide-   398    trans-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   399    cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   400    trans-1-(2,4dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   401    cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1-pyrazole-3-carbothioamide-   402    trans-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   403    cis-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   404    trans-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   405    cis-1-(2-chlorophenyl)-5(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   406    trans-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide-   407    7-(4-Chloro-phenyl)-6(2,4-dichlorophenyl)-5,6-diaza-spiro[2.4]hept-4-ene-4-carboxylic    acid piperidin-1-ylamide-   408    6-(2,4-Dichloro-phenyl)-7-(4-methoxy-phenyl)-5,6-diaza-spiro[2.4]hept-4-ene-4-carboxylic    acid piperidin-1-ylamide-   409 (+)-(c)-N-((1S,2S)-2-(benzyloxy    cyclohexyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5dihydro-1H-pyrazole-3-carboxamide-   [410]    cis-1-(2,4dichlorophenyl)-5-(4-ethoxyphenyl)-4methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   [411]    cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   [412]    (4R,5S)-1-(2,4dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   [413]    cis-5-(4-bromophenyl)-1-(2,4dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3carboxylic    acid-   [414]    cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   415    cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   416 trans-ethyl    5-(4-chlorophenyl)-1-(2,4dichlorophenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole    3carboxylate-   417    cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   418    cis-5-(4bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   419    (−)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   420    (+)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   421 trans-ethyl    1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylate-   422    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-((1R,2S,4R)-1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   423    cis-5-(4chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(3-methylcyclohexyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   424    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(2-methylcyclohexyl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   426    trans-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   427    cis-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   428    cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   [429]    1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid-   [430]    cis-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    hydrochloride-   [431]    trans-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   432    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   434    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide-   436    (+)-cis-N-((1S,2S)-2-(benzyloxy)cyclohexyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   -437    (−)-cis-N-((1R,2R)-2-(benzyloxy)cyclohexyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   438    cis-N-(azocan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   439    cis-N-(azocan-1-yl)-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   440    cis-N-(azocan-1-yl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   441    cis-N-(azocan-1-yl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   442    cis-N-(azocan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   443    cis-N-(azocan-1-yl)-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide-   444    (+)-cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid azepan-1-ylamide hydrochloride-   445    (−)-cis-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic    acid azepan-1-ylamide hydrochloride-   [446]    cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    N-oxide-   [447]    cis-5-(4-chlorophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    N-oxide-   [448]    cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    N-oxide-   [449]    cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide    N-oxide-   [450]    cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    N-oxide and-   [451]    cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide    N-oxide;    optionally in form of one of its stereoisomers, preferably    enantiomers or diastereomers, a racemate or in form of a mixture of    at least two of its stereoisomers, preferably enantiomers and/or    diastereomers, in any mixing ratio, or a corresponding N-oxide    thereof, or a physiologically acceptable salt thereof, or a    corresponding solvate thereof.

In another aspect the present invention also provides a process for thepreparation of 4-substituted pyrazoline compounds of general formula Igiven above, wherein R⁵ represents hydrogen, according to which at leastone compound of general formula II,

wherein R¹, X and R⁴ have the meaning given above, is reacted with atleast one compound of general formula III,

or a corresponding salt thereof, wherein R² has the meaning given above,in a reaction medium, optionally in an inert atmosphere, optionally inthe presence of at least one acid, to yield at least one compound ofgeneral formula IV,

wherein R¹, X, R² and R⁴ have the meaning given above, which isoptionally isolated and/or purified,and at least one compound of general formula IV is reacted with anactivating agent in a reaction medium, optionally in an inertatmosphere, to yield at least one compound of general formula V,

wherein R¹, X, R² and R⁴ have the meaning according given above and Arepresents a leaving group, which is optionally purified and/orisolated,and at least one compound of general formula V is reacted with at leastone compound of general formula R³—H, wherein R³ has the meaning givenabove, in a reaction medium, optionally in an inert atmosphere,optionally in the presence of at least one base selected from the groupconsisting of diisopropylethylamine, triethylamine, pyridine,dimethylaminopyridine and N-methylmorpholine, to yield at least onecompound of general formula I, wherein R¹, R², X, R³ and R⁴ have themeaning given above and R⁵ represents hydrogen, which is optionallypurified and/or isolated;or at least one compound of general formula IV is reacted with at leastone compound of general formula R³—H, wherein R³ represents a —NR⁷R⁸moiety, whereby R⁷ and R⁸ have the meaning given above, in a reactionmedium, in the presence of at least one coupling agent, optionally inthe presence of at least one base, to yield at least one compound ofgeneral formula I, wherein R¹, R², X and R⁴ have the meaning givenabove, R³ represents a —NR⁷R⁸ moiety and R⁵ represents hydrogen, whichis optionally purified and/or isolated.

Also preferred is the process for the preparation of a compound ofgeneral formula I given above, wherein R⁵ represents a hydrogen atom,according to which at least one compound of general formula R¹—C(═O)—H(general formula VII), wherein R¹ has the meaning given above, isreacted with at least one compound of general formula VI,

wherein R⁴ and X have the meaning given above and R¹ represents a linearor branched C₁₋₆-alkyl radical, preferably an ethyl radical, a potassiumcation or a sodium cation, in a reaction medium, optionally in an inertatmosphere, optionally in the presence of at least one base, to yield atleast one compound of general formula II,

wherein R¹, X and R⁴ have the meaning given above, which is optionallypurified and/or isolated,and at least one compound of general formula II is reacted with anactivating agent in a reaction medium, optionally in an inertatmosphere, to yield at least one compound of general formula VII,

wherein R¹, X and R⁴ have the meaning given above and A represents aleaving group, which is optionally purified and/or isolated,and at least one compound of general formula VII is reacted with atleast one compound of general formula R³—H, wherein R³ has the meaninggiven above, in a reaction medium, optionally in an inert atmosphere,optionally in the presence of at least one base selected from the groupconsisting of diisopropylethylamine, triethylamine, pyridine,dimethylaminopyridine and N-methylmorpholine, to yield at least onecompound of general formula IX,

wherein R¹, X, R³ and R⁴ have the meaning given above, which isoptionally purified and/or isolated;or at least one compound of general formula II is reacted with at leastone compound of general formula R³—H, wherein R³ represents a —NR⁷R⁸moiety, whereby R⁷ and R⁸ have the meaning given above, in a reactionmedium, in the presence of at least one coupling agent, optionally inthe presence of at least one base, to yield at least one compound ofgeneral formula IX, wherein R³ represents a —NR⁷R⁸ moiety, which isoptionally purified and/or isolated,and at least one compound of general formula IX is reacted with at leastone compound of general formula III,

wherein R² has the meaning given above, in a reaction medium, optionallyin an inert atmosphere, optionally in the presence of at least one acid,to yield a compound of general formula I, wherein R¹, X, R², R³ and R⁴have the meaning given above and R⁵ represents hydrogen, which isoptionally purified and/or isolated.

The inventive process is also illustrated in scheme I given below:

In step 1 a compound of general formula VI is reacted with a compound ofgeneral formula VII in a protic reaction medium, preferably in areaction medium selected from the group consisting of methanol, ethanol,isopropanol, n-butanol, water and mixtures thereof, in the presence ofat least one base, preferably in the presence of an alkali metalhydroxide such as sodium hydroxide or potassium hydroxide or an alkalimetal methoxide such as sodium methoxide, as described, for example, inSynthetic Communications, 26(11), 2229-33, (1996). The respectivedescription is hereby incorporated by reference and forms part of thedisclosure. Reaction temperature as well as the duration of the reactionmay vary over a broad range. Preferred reaction temperatures range from−10° C. to the boiling point of the reaction medium. Suitable reactiontimes may vary for example from several minutes to several hours.

Preferably the reaction between a compound of general formula VI andgeneral formula VII can also be carried out under acid catalysedconditions, more preferably by refluxing the above mentioned compoundsin dichloromethane in the presence ofcopper(II)trifluoromethanesulfonate as described, for example, inSynlett, (1), 147-149, 2001. The respective description is herebyincorporated by reference and forms part of the disclosure.

In step 2 a compound of general formula II is reacted with a compound ofgeneral formula III in a reaction medium, preferably in a reactionmedium selected from the group consisting of methanol, ethanol,isopropanol, n-butanol, diethylether, tert-butyl-methylether, dioxane,Tetrahydrofuran or mixtures of at least two of these afore mentionedreaction media. Also preferably, said reaction may be carried out in thepresence of an acid, whereby the acid may be organic such as acetic acidand/or inorganic such as hydrochloric acid. Alternatively the reactionmay also be carried out in the presence of a base such as piperidine,piperazine, sodium hydroxide, potassium hydroxide, sodium methoxide orsodium ethoxide or mixtures of at least two of these bases.

Reaction temperature as well as the duration of the reaction may varyover a broad range. Suitable reaction temperatures range from roomtemperature, i.e. approximately 25° C. to the boiling point of thereaction medium. Suitable reaction times may vary for example fromseveral minutes to several hours. This reaction preferably leads toracemates of compounds of general formula IV, wherein the substituentsR¹ and R⁴ are located cis to one another on the pyrazoline ring. Therespective enantiomers can be separated by conventional methodsincluding chiral HPLC or resolution via the formation of diastereomericsalts and thus leading to compounds of general formula IV with anee>99%. The configuration of compounds of general formula IV ismaintained during the subsequent reaction steps, thus leading toenantiomerically pure compounds of general formula I (ee>99%). In step 2racemates of compounds of general formula IV, wherein the substituentsR¹ and R⁴ are located trans to one another on the pyrazoline ring, arealso formed, albeit in a low yield.

In step 3 the carboxylic group of the compound of general formula IV maybe activated for further reactions by the introduction of a suitableleaving group according to conventional methods well known to thoseskilled in the art. Preferably the compounds of general formula IV aretransferred into an acid chloride, an acid anhydride, a mixed anhydride,a C₁₋₄ alkyl ester or an activated ester such as p-nitrophenylester.Suitable activating agent therefore are selected from the groupconsisting of thionyl chloride, oxalyl chloride and ethylchloroformate.

If said activated compound of general formula V is an acid chloride,wherein A represents a chlorine atom, that compound is preferablyprepared by the reaction of the corresponding acid of general formula IVwith thionyl chloride or oxalyl chloride, whereby said chlorinatingagent is also used as the reaction medium, in the presence of at leastone base, preferably in the presence of a base selected from the groupconsisting of triethylamine, N-methylmorpholine, pyridine,dimethylaminopyridine and diisopropylethylamine. Also preferably anadditional reaction medium may be used. Suitable reaction media includehydrocarbons such as benzene, toluene or xylene, halogenatedhydrocarbons such as dichloromethane, chloroform or carbontetrachloride, ethers such as diethyl ether, dioxane, Tetrahydrofuran ordimethoxyethane or dimethylformamide and mixtures thereof. Morepreferably toluene in the presence of a catalytic amount ofdimethylformamide is used as reaction medium. Preferred reactiontemperature range from 0° C. to the boiling point of the solvent andreaction times vary from several minutes to several hours.

If said activated compound of general formula V is a mixed anhydride,wherein A represents —O—C(═O)—O—C₂H₅, said anhydride may preferably beprepared, for example, by reaction of the corresponding acid of generalformula IV with ethylchloroformate in the presence of a base such astriethylamine, pyridine or diisopropylethylamine, in a suitable solventsuch as dichloromethane, optionally in an inert atmosphere, at atemperature between −50° C. and 50° C.

In step 4 the reaction between a compound of general formula V with acompound of general formula H—R³ to yield a compound of general formulaI, wherein R³ represents a —NR⁷R⁸ moiety, is preferably carried out inthe presence of a base such as triethylamine in a reaction medium suchas methylenchloride. The temperature is preferably in the range from 0°C. to the boiling point of the reaction medium. The reaction time mayvary over a broad range, e.g. from several hours to several days.

Alternatively the reaction of a compound of general formula V with acompound of general formula H—R³ to yield compounds of general formula Imay be carried out according to conventional methods well known to thoseskilled in the art, e.g. from Pascual, A., J. Prakt Chem., 1999, 341(7),695-700; Lin, S. et al., Heterocycles, 2001, 55(2), 265-277; Rao, P. etal., J. Org. Chem., 2000, 65(22), 7323-7344, Pearson D. E and Buehler,C. A., Synthesis, 1972, 533-542 and references cited therein. Therespective descriptions are hereby incorporated by reference and formpart of the present disclosure.

Preferably said reaction is carried out in the presence of a Lewis acid,which is preferably selected from the group consisting of FeCl₃, ZnCl₂and AlCl₃, in a suitable reaction medium such as toluene, benzene,Tetrahydrofuran or similar reaction media. The temperature is preferablyin the range from 0° C. to the boiling point of the reaction medium,more preferably from 15 to 25° C. The reaction time may vary over abroad range, e.g. from several minutes to several hours.

In step 5 a compound of general formula IV is reacted with a compound ofgeneral formula H—R³, wherein R³ represents a —NR⁷R⁸ moiety, in areaction medium, preferably in a reaction medium selected from the groupconsisting of diethylether, Tetrahydrofuran, acetonitrile, methanol,ethanol, (1,2)-dichlorethane, dimethylformamide, dichlormethane andmixtures thereof, in the presence of at least one coupling agent,preferably in the presence of a coupling agent selected from the groupconsisting of 1-benzotriazolyloxy-tris-(dimethylamino)-phosphoniumhexafluorophosphate (BOP), dicyclohexylcarbodiimide (DCC),N′-(3-dimethylaminopropyl)-N-ethylcarbodiimide (EDCI),diisoproylcarbodiimide, 1,1′-carbonyl-diimidazole (CDI),N-[(dimethyamino)-1H-1, 2, 3-triazolo[4,5-b]pyridino-1-ylmethylen]-N-methylmethanaminium hexafluorophosphateN-oxid (HATU), O-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluroniomhexafluorophosphate (HBTU),O-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium-tetrafluoroborate(TBTU), 1-hydroxy-benzotriazole (HOBt) and 1-hydroxy-7-azabenzotriazol(HOAt), optionally in the presence of a base, preferably in the presenceof a base selected from the group consisting of pyridine,dimethylaminopyridine, N-methylmorpholine, triethylamine anddiisopropylethylamine to yield a compound of general formula I, whereinR³ represents a —NR⁷R⁸ moiety.

Preferably said reaction is carried out in the presence of EDCI andHOBt, optionally in the presence of N-methylmorpholine or triethylamine,in an aprotic reaction medium such as dimethylformamide orTetrahydrofuran, at a temperature between 20° C. and 30° C. for 15 to 24hours as described in Tetrahedron Lett. 2004, 45, 4977. The respectivedescription is hereby incorporated by reference and forms part of thedisclosure. Polymer-supported EDCI (P-EDCI) can also suitably be usedfor this process instead of EDCI as described in Tetrahedron Lett. 1998,39, 1487 and Tetrahedron Lett. 2002, 43, 7685. The respectivedescriptions are hereby incorporated by reference and form part of thedisclosure.

Alternatively said reaction can be carried out by using HBTU in thepresence of a base such as diisopropylethylamine in an aprotic solvent,such as acetonitrile, preferably at a temperature between 20 and 30° C.for 15 to 24 hours.

A further inventive process to obtain compounds of general formula IV isillustrated in scheme II given below.

In step 1 a compound of general formula XI, wherein R¹, R⁴ and X havethe meaning given above and R″ represents a hydrogen atom or a C₁₋₆alkyl radical, is reacted with a compound of general formula HS—R′″,wherein R′″ represents an unsubstituted or at least mono-substitutedphenyl radical, in a reaction medium, preferably in an dry aproticreaction medium, more preferably in toluene, optionally in the presenceof an organic base, preferably in the presence of an organic baseselected from the group consisting of triethylamine, pyridine,diisopropylethylamine, dimethylaminopyridine and N-methylmorpholine,preferably at a temperature between −50° C. and 50° C., preferably for 4to 24 hours, to yield a compound of general formula XII, wherein R¹, R⁴,R″, R′″ and X have the meaning given above.

In step 2 a compound of general formula XII is reacted with a compoundof general formula III, wherein R² has the meaning given above, in areaction medium, preferably in a protic reaction medium, more preferablyin methanol, optionally in the presence of an inorganic base, preferablyin the presence of KHSO₄, preferably at a temperature between 0° C. and100° C., preferably for 4 to 15 hours, to yield a compound of generalformula XIII, wherein R¹, R², R⁴, R″, R′″ and X have the meaning givenabove.

In step 3 the compound of general formula XIII is cyclizedintramolecularly in a reaction medium, preferably in a dry aproticreaction medium, more preferably in dimethylformamide, preferably underan inert atmosphere, in the presence of a base, preferably in thepresence of a metal hydride salt, more preferably in the presence ofsodium hydride and/or potassium hydride to yield a compound of generalformula IV. If R″ represents a C₁₋₆-alkyl radical, the compound ofgeneral formula IV, wherein R″ represents a hydrogen atom, is obtainedafter saponification of the cyclized compound according to methods knownto those skilled in the art.

The sequence illustrated in scheme 1 is also described in, for example,Tetrahedron 2005, 81, 5235-5240 and Tetrahedron Asymmetry 2001, 12,1923-1928. The respective descriptions are hereby incorporated byreference and form part of the disclosure.

A compound of general formula IV can also be obtained as described inscheme III given below.

The compound of general formula XIV, wherein R¹, R⁴ and X have themeaning given above and R″ represents a hydrogen atom or a C₁₋₆-alkylradical, is obtained by the bromination of a compound of general formulaXI in a reaction medium, preferably in an aprotic reaction medium, morepreferably in dichloromethane, with bromine at a temperature between 0°C. and 30° C. for several hours as described in Tetrahedron Lett. 1998,39 (44), 8163-8166; J. Chem. Soc. Perkin Trans 1, 1999, 21, 3069-3070;Tetrahedron 1999, 55 (36), 11127-11142 and J. Heterocyclic Chem. 1986,23, 1199. Preferably a compound of general formula XIV is reacted withbromine in the presence of an aprotic solvent, preferably in thepresence of dichloromethane, at ambient temperature for 1 to 2 hours.The respective descriptions are hereby incorporated by reference andform part of the disclosure.

The compound of general formula XIV is reacted with a compound ofgeneral formula III, wherein R² has the meaning given above, andcyclized intramolecularly in a reaction medium, preferably in a dryaprotic reaction medium, more preferably in dimethylformamide or in amixture of dioxane, water and acetic acid, at a temperature between 0°C. and 250° C. to yield a compound of general formula IV as described inChemistry of Heterocyclic Compounds 1997, 33(6); Indian J. Chem. 20B,1981, 1090; Indian J. Chem. 29B, 1990, 887 and J. Indian Chem. Soc.1997, 74(3), 202-205. The respective descriptions are herebyincorporated by reference and form part of the disclosure. If R″represents a C₁₋₆-alkyl radical, the compound of general formula IV,wherein R″ represents a hydrogen atom, is obtained after saponificationof the cyclized compound according to methods known to those skilled inthe art.

A compound of general formula IV can also be obtained by the processdescribed in scheme IV.

An aldehyde of general formula VII, wherein R¹ has the meaning givenabove, is reacted with either a phosphonium ylide of general formula XV,a phosphine oxide of general formula XVI or a phosphonate of generalformula XVII, wherein in each case R⁴ and X have the meaning givenabove, R″ represents a hydrogen atom or a C₁₋₆-alkyl radical and Zrepresents an unsubstituted or at least mono-substituted phenyl radical,in a reaction medium, preferably in an aprotic reaction medium, morepreferably in Tetrahydrofuran, optionally in the presence of at leastone base, preferably in the presence of a base selected from the groupconsisting of potassium tert-butylat, n-butyllithium, sodium hydride andlithium diisopropylamide, to yield a compound of general formula XIwhich is reacted with a compound of general formula III, wherein R² hasthe meaning given above, and cyclized intramolecularly to yield acompound of general formula IV as described above. The process is alsodescribed in Tetrahedron 1994, 50 (44), 12727-12742 and Zhurnal ObshcheiKhimii 1986, 56 (2), 347-353. The respective descriptions are herebyincorporated by reference and form part of the disclosure. If R″represents a C₁₋₆-alkyl radical, the compound of general formula IV,wherein R″ represents a hydrogen atom, is obtained after saponificationof the cyclized compound according to methods known to those skilled inthe art.

Another method for the preparation of compounds of general formula XI isillustrated in scheme V below.

A compound of general formula VII, wherein R¹ has the meaning givenabove, is reacted with a phosphonate of general formula XVIII, whereinR⁴ has the meaning given above and R″″ represents a C₁₋₆-alkyl radical,preferably an ethyl radical, and a compound of general formula XIX,wherein X has the meaning given above and R″ represents a hydrogen atomor a C₁₋₆-alkyl radical to yield a compound of general formula XI,wherein R¹, R⁴, X and R″ have the meaning given above. The process isdescribed in J. Chem. Soc. Perkin Trans 1, 1995, 741-742. Preferably thereaction is carried out by the addition of phosphonate of generalformula XVIII to a solution of n-butyllithium in a dry reaction medium,preferably in Tetrahydrofuran, at a temperature between −100° C. and−50° C., followed by the addition of N-phenylalcoxycarbonylacetimidoylchloride of general formula XIX and aldehyde of general formula VII andstirring at a temperature between 0° C. and 30° C. for several hours.The respective description is hereby incorporated by reference and formspart of the disclosure.

A compound of general formula IV can also be obtained according to theprocess described in scheme VI.

A compound of general formula VII, wherein R¹ has the meaning givenabove, is reacted with a compound of general formula XX, wherein R², R⁴and X have the meaning given above and R″″ represents a C₁₋₆-alkylradical, is reacted in a reaction medium, preferably in ethanol, in thepresence of a base, preferably sodium acetate, at a temperature between30° C. and 90° C., or in a reaction medium, preferably in ethanol, inthe presence of glacial acetic acid at a temperature between 0° C. and50° C. to yield a compound of general formula XXI, wherein R¹, R², R⁴and X have the meaning given above and R″″ represents a C₁₋₆-alkylradical. The compound of general formula XXI is converted into thecompound of general formula IV in a reaction medium, preferably inethanol and/or water, in the presence of an acid, preferably in thepresence of hydrochloric acid, at a temperature between 50° C. and 120°C. to yield a compound of general formula IV. The process is describedin J. Chem. Engineering Data 1984, 29(2), 225-229 and Indian J. Chem.27B, 1988, 3, 245-249. The respective descriptions are herebyincorporated by reference and form part of the disclosure.

A compound of general formula IV can also be obtained according to theprocess described in scheme VII. Said process is also described inWO88/005046. The respective description is hereby incorporated byreference and forms part of the disclosure.

A compound of general formula XXII, wherein R¹ and R⁴ have the meaninggiven above, is reacted with a compound of general formula XXIII,wherein R² and X have the meaning given above, R″″ represents aC₁₋₆-alkyl radical and Y represents a chlorine or bromine atom, in areaction medium, preferably in an aprotic or protic reaction medium,more preferably in toluene and/or chloroform and/or ethanol, in thepresence of a base, preferably an organic base, more preferably anorganic base selected from the group consisting of triethylamine,pyridine, diisopropylethylamine, dimethylaminopyridine,1,4-diazabicyclo[2.2.2]octane and N-methylmorpholine, at a temperaturebetween 0° C. and 150° C. to yield a compound of general formula IV. Ifregioisomers are obtained during the reaction, these regioisomers can beseparated by conventional chromatographic techniques. The compound ofgeneral formula IV, wherein R″″ represents a C₁₋₆-alkyl radical isconverted into the corresponding acid by using standard methods whichare known to those skilled in the art. The process is disclosed in Bull.Chem. Soc. Japan 1984, 57 (3), 787-790 and Chem. Lett. 1982, 543-546.The respective descriptions are hereby incorporated by reference andform part of the disclosure. The method as depicted in scheme VII isstereospecific. Thus, using (E)-olefins of general formula XII compoundsof general formula IV are obtained, wherein the radicals R¹ and R⁴ onthe pyrazoline ring are orientated trans to one another. Starting from(Z)-olefins the respective pyrazolines with cis-configuration areobtained. The racemates of pyrazoline compounds with either trans- orcis-configuration can be separated by conventional methods includingchiral HPLC separation and separation via the formation ofdiastereomeric salts. Thus, enantiomerically pure compounds are obtained(ee>99%). The configuration of compounds of general formula IV ismaintained during the subsequent reaction steps, thus leading toenantiomerically pure compounds of general formula I (ee>99%).

The compound of general formula XXIII can be prepared according to theprocesses described in scheme VIII.

The compound of general formula XXIV, wherein X has the meaning givenabove and R″″ represents a C₁₋₆-alkyl radical, is reacted in a reactionmedium, preferably in a mixture of water and ethanol, in the presence ofat least one acid, preferably in the presence of acetic acid, at atemperature between 70° C. and 120° C. with a compound of generalformula III, wherein R² has the meaning given above, to yield a compoundof general formula XXV, wherein R² and X have the meaning given aboveand R″″ represents a C₁₋₆-alkyl radical, which is reacted withN-chloro-succinimide or N-bromo-succinimide in a reaction medium,preferably in an aprotic reaction medium, more preferably indimethylformamide, at a temperature between 0° C. and 30° C., to yield acompound of general formula XXIII. The process is described in Synth.Commun. 2001, 31(1), 111-115 and Tetrahedron 1994, 50 (25), 7543-7556.The respective descriptions are hereby incorporated by reference andform part of the disclosure.

The compound of general formula XXIII can also be prepared by thereaction of a compound of general formula XXVI, wherein X has themeaning given above and R″″ represents a C₁₋₆-alkyl radical, with acompound of general formula XXVII, wherein R² has the meaning givenabove and subsequent bromination of the resulting compound of generalformula XXVIII, wherein R² and X have the meaning given above and R″″represents a C₁₋₆-alkyl radical, by using bromine in the presence ofacetic acid as described in Synthesis 1975, 333 and J. Chem. Soc. PerkinTrans. 1, 1977, 2092. The diazonium salt of general formula XXVII canpreferably be obtained by the addition of an aqueous solution of sodiumnitrite to a compound of general formula R²—NH₂ in aqueous hydrochlorideacid, wherein R² has the meaning given above. Alternatively thistransformation can also be achieved in the presence of a compound ofgeneral formula XXVI by adjusting the pH of the reaction medium to 4 bythe addition of sodium acetate at a temperature between 0° C. and 30° C.The respective descriptions are hereby incorporated by reference andform part of the disclosure.

The compound of general formula XXIII can also be prepared by thereaction of a compound of general formula XXIX, wherein X has themeaning given above, R″″ represents a C₁₋₆-alkyl radical and Yrepresents a chlorine or bromine atom, with dimethylsulfide, in areaction medium, preferably in ethanol, at a temperature between 70° C.and 120° C. Optionally the dimethylsulfonium salt is isolated andfurther reacted with a compound of general formula XXVII, wherein R² hasthe meaning given above, in the presence of sodium acetate and aceticacid at a temperature between 0° C. and 30° C. as described inHeterocycles 1991, 32(6), 1101-1107. The respective description ishereby incorporated by reference and forms part of the disclosure.

The compound of general formula XXIII can also be prepared by thereaction of a compound of general formula XXXXVIII, wherein X has themeaning given above, R″″ represents a C₁₋₆-alkyl radical and Yrepresents a leaving group, preferably a leaving group selected from thegroup consisting of chlorine and bromine, with a compound of generalformula XXVII, wherein R² has the meaning given above, in the presenceof a protic solvent, preferably in the presence of a protic solventselected from the group consisting of methanol and ethanol, or in thepresence of an aprotic solvent, preferably in the presence oftetrahydrofuran, in the presence of a base, preferably in the presenceof sodium acetate, or in the presence of an acid, preferably in thepresence of acetic acid. The method is described in J. Chem. Soc. PerkinTransaction 1 1998, 24, 4103-4106; Tetrahedron Asymmetry 2000, 11(9),1975-1983; Tetrahedron 1998, 54(49), 14859-14868; Synthesis 1996, 9,1076-1078 and Synthesis 1995, 12, 1483-1484. The respective descriptionsare hereby incorporated by reference and form part of the disclosure.

Another method for the preparation of a compound of general formula IVis described in scheme IX.

A compound of general formula XXX, wherein R² and X have the meaninggiven above, Z represents an unsubstituted or at least mono-substitutedphenyl radical, preferably an unsubstituted phenyl radical, and R″″represents a C₁₋₆-alkyl radical, preferably an ethyl radical, is reactedwith a compound of general formula XXII, wherein R¹ and R⁴ have themeaning given above, in a reaction medium, preferably in xylene, at atemperature between 50° C. and 200° C. for 2 to 30 hours to yield acompound of general formula IV. The process is described in Chem. Lett.1983, 507-510 and Bull. Chem. Soc. Japan 1984, 57(9), 2689-2690. Therespective descriptions are hereby incorporated by reference and formpart of the disclosure.

The compound of general formula IV, wherein R″″ represents a C₁₋₆-alkylradical, is converted into the corresponding acid by using standardmethods which are known to those skilled in the art.

A process for the preparation of a compound of general formula XXX isdescribed in scheme X.

A compound of general formula XXXI, wherein X has the meaning givenabove and R″″ is a C₁₋₆-alkyl radical, is reacted with a compound ofgeneral formula III, wherein R² has the meaning given above, to yield acompound of general formula XXXII, wherein R² and X have the meaninggiven above and R″″ represents a C₁₋₆-alkyl radical. Subsequently, thecompound of general formula XXXIII is reacted with phosphorouspentachloride or POCl₃ in a reaction medium, preferably in toluene, at atemperature between 0° C. and 50° C., followed by the addition of aphenolic compound, preferably O-trimethylsilyl-p-cresol, in refluxingtoluene to yield a compound of general formula XXX.

Another method for the preparation of a compound of general formula IVis described in scheme XI.

A compound of general formula XXXIII, wherein R¹ and R⁴ have the meaninggiven above and W represents —C(═X)—OH, —C(═X)—OR″″ or —CN, whereby Xhas the meaning given above and R″″ represents a C₁₋₆-alkyl radical, isconverted to a compound of general formula XXXIV, wherein R¹, R⁴ and Whave the meaning given above, by means of epoxidation with a reagentselected from the group consisting of perbenzoic acid, preferablym-chloro-perbenzoic acid, sodium peroxocarbonate, hydrogen peroxide,dioxirane and hydroperoxide. The compound of general formula XXIV isreacted with a compound of general formula III, wherein R² has themeaning given above, in a reaction medium, preferably in ethanol, toyield a compound of general formula XXXV, wherein R¹, R², W and R⁴ havethe meaning given above. Subsequently, the compound of general formulaXXXV is converted into the corresponding xanthate of general formulaXXXVI, wherein R¹, R², W and R⁴ have the meaning given above, byreaction with an unsubstituted or at least mono-substitutedphenylthionochloroformate of general formula ZO—C(═S)—Cl, wherein Zrepresents an unsubstituted or at least mono-substituted phenyl radical.The compound of general formula XXXVI is reacted with tributyltinhydrideoptionally followed by saponification and/or hydrolysis to yield acompound of general formula IV, wherein R¹, R², X and R⁴ have themeaning given above. The process is. described in Synlett 1990, 11,705-706. The respective description is hereby incorporated by referenceand forms part of the disclosure.

Yet another method for the preparation of a compound of general formulaIV is described in scheme XII.

A compound of general formula XXXVII, wherein R² has the meaning givenabove, is reacted with a compound of general formula XXXVIII, wherein R⁴and X have the meaning given above and R″ represents a hydrogen atom ora C₁₋₆-alkyl radical, and a compound of general formula VII, wherein R¹has the meaning given above, to yield a compound of general formulaXXXIX, wherein R¹, R², R⁴ and X have the meaning given above and R″represents a hydrogen atom or a C₁₋₆-alkyl radical. The compound ofgeneral formula XXXIX is converted into the compound of general formulaXXXX by using O-substituted hydroxylamines according to the methoddescribed in J. Org. Chem. 2002, 67, 6237-6239. The respectivedescription is hereby incorporated by reference and forms part of thedisclosure. Alternatively, this transformation can be achieved by usingnitrites and subsequent reduction according to methods known to thoseskilled in the art. Upon cyclization of a compound of general formulaXXXX according-to the methods described above a compound of generalformula IV is obtained. If R″ represents a C₁₋₆-alkyl radical, thecompound of general formula IV, wherein R″ represents hydrogen, isobtained after saponification of the cyclized compound according tomethods known to those skilled in the art.

In case R⁵ is unlike hydrogen the reaction sequence given in Scheme I isadapted as follows.

In step 1 a compound of general formula VIb or a corresponding enolateof said compound is reacted with a compound of general formula VII in areaction medium, preferably in a protic reaction medium, more preferablyin a reaction medium selected from the group consisting of methanol,ethanol, isopropanol, n-butanol, water and mixtures thereof, in thepresence of at least one base, preferably in the presence of an alkalimetal hydroxide such as sodium hydroxide or potassium hydroxide or analkali metal methoxide such as sodium methoxide or in the presence oflithium diisopropylamide in an aprotic solvent, preferably intetrahydrofuran.

In step 2 a compound of general formula XXXXI is transformed into acompound of general formula XXXXII which contains a good living groupLG, preferably a leaving group selected from the group consisting ofmesyl and tosyl, using conventional methods known to those skilled inthe art.

In step 3 a compound of general formula XXXXII is reacted with acompound of general formula III in a reaction medium, preferably in areaction medium selected from the group consisting of methanol, ethanol,isopropanol, n-butanol, diethylether, tert-butyl-methylether, dioxane,tetrahydrofuran or mixtures of at least two of these afore mentionedreaction media. Also preferably, said reaction may be carried out in thepresence of an acid, whereby the acid may be organic such as acetic acidand/or inorganic such as hydrochloric acid. Alternatively the reactionmay also be carried out in the presence of a base such as piperidine,piperazine, sodium hydroxide, potassium hydroxide, sodium methoxide orsodium ethoxide or mixtures of at least two of these bases. Reactiontemperature as well as the duration of the reaction may vary over abroad range. Suitable reaction temperatures range from room temperature,i.e. approximately 25° C. to the boiling point of the reaction medium.Suitable reaction times may vary for example from several minutes toseveral hours.

Step 4 can be carried out as described for step 3, scheme I; step 5 canbe carried out as described for step 4, scheme I and step 6 can becarried out as described for step 5, scheme 1.

The compounds of general formula 1, wherein R⁵ is unlike hydrogen, canalso be obtained by the reaction sequence described in scheme XIV.

The reaction is carried out as described for the analogues reactiondepicted in scheme VII. If a mixture of regioisomers is obtained, saidregioisomers can be separated by standard methods known to those skilledin the art, e. g. chromatographic methods or crystallization. Theprocess is disclosed in Bull. Chem. Soc. Japan 1984, 57 (3), 787-790.The respective description is hereby incorporated by reference and formspart of the disclosure. The compounds of general formula I, wherein R³represents —NR⁷R⁸, can also be obtained by the reaction sequencedescribed in scheme XV.

In step 1 a compound of general formula V is reacted with hydrazinehydrate in the presence of an aprotic or protic solvent, preferably inthe presence of ethanol, at reflux temperature to yield a compound ofgeneral formula XXXXIII, wherein R¹, R², R⁴ and X have the meaning asdefined above.

In step 2 a compound of general formula XXXXIII is reacted with acompound of general formula XXXXIV, wherein R represents a hydrogen atomor a linear or branched C₁₋₁₂alkyl radical and n is 0, 1, 2, 3, 4, 5, 6,7, 8, 9 or 10, in the presence of benzotriazole to yield a compound ofgeneral formula XXXXV, wherein R, n, R¹, R², R⁴ and X have the meaningas defined above and Bt represents a benzotriazolyl radical. A compoundof general formula XXXXV can be transformed into a compound of generalformula XXXXVI, wherein R, n, R¹, R², R⁴ and X have the meaning asdefined above, in the presence of a reducing agent, preferably in thepresence of sodium borohydride, in the presence of an aprotic solvent,preferably in the presence of tetrahydrofuran. Alternatively, thebenzotriazole moiety in compounds of general formula XXXXV can bereplaced by a linear or branched C₁₋₁₀alkyl group via reaction with therespective alkyl Grignard reagents The process is disclosed J. Org.Chem. 1990, 55, 3205-3209. The respective description is herebyincorporated by reference and forms part of the disclosure.

The compounds of general formula 1, wherein R³ represents —NR⁷R⁸, canalso be obtained by the reaction sequence described in scheme XVI.

Scheme XVI.

In step 1 a compound of general formula XXXXIII is reacted with acompound of general formula XXXXIV, wherein R represents a hydrogen atomor a linear or branched C₁₋₁₂alkyl radical and n is 0, 1, 2, 3, 4, 5, 6,7, 8, 9 or 10, in the presence of a reducing agent, preferably in thepresence of a reducing agent selected from the group consisting ofsodium borohydride, sodium cyanoborohydride or triacetoxyborohydride, toyield a compound of general formula XXXXVI, wherein R, n, R¹, R², R⁴ andX have the meaning as defined above.

In step 2 a compound of general formula XXXXIII is reacted with acompound of general formula XXXXVII, wherein R represents a hydrogenatom or a linear or branched C₁₋₁₂alkyl radical, n is 0, 1, 2, 3, 4, 5,6, 7, 8, 9 or 10 and LG represents a leaving group, preferably a leavinggroup selected from the group consisting of chlorine and bromine, morepreferably LG represents bromine, in the presence of a base, preferablyin the presence of potassium carbonate, to yield a compound of generalformula XXXXVI, wherein R, n, R¹, R², R⁴ and X have the meaning asdefined above.

The compounds of general formula I can also be obtained by the reactionsequence described in scheme XVII.

A compound of general formula IV, wherein R⁴ represents hydrogen and R¹,R² and X have the above defined meaning, is transformed into a compoundof general formula IV, wherein R⁴ is unlike hydrogen and R¹, R², R⁴ andX have the above defined meaning, in the presence of a base, preferablyin the presence of a base selected from the group consisting of sodiumhydride, lithium diisopropylamide and lithium hexamethyldisilazide, inthe presence of an aprotic solvent, preferably in the presence of anaprotic solvent selected from the group consisting of tetrahydrofuran,dichloromethane and chloroform, and in the presence of a compound ofgeneral formula R⁴—X, wherein R⁴ has the above defined meaning,preferably R⁴ represents a linear or branched C₁₋₁₀alkyl radical or CN,and X represents a leaving group, preferably a leaving group selectedfrom the group consisting of bromine and iodine. The compounds ofgeneral formula IV, wherein R⁴ is unlike hydrogen, are obtained asracemates, and can be separated by conventional methods including HPLCand separation via formation of diastereomeric salts. The compounds ofgeneral formula IV can be transformed into compounds of general formulaI while retaining the absolute configuration of the compounds of generalformula 1.

A compound of general formula IV, wherein both R⁴ and R⁵ are differentfrom hydrogen and R¹, R⁴, R² and X have the above defined meaning, canbe prepared from compounds of general formula IV, wherein R⁵ ishydrogen, R⁴is unlike hydrogen and R¹, R⁴, R² and X have the abovedefined meaning, and a compound of general formula R⁵—X, wherein R⁵ hasthe above defined meaning, preferably R⁵ represents a linear or branchedC₁₋₁₀alkyl radical or CN, and X represents a leaving group, preferably aleaving group selected from the group consisting of bromine and iodine,by applying the same method as described in scheme XVII.

Compounds of general formula I, wherein X represents O, can betransformed in the corresponding compound, wherein X represents S, byreacting the first compound with a dithiaphosphetane, preferably with2,4-bis(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetan-2,4-disulfide(Lawesson reagent) or phosphorous pentasulfide, in a reaction medium,preferably in a reaction medium selected from the group consisting oftoluene, xylene, acetonitrile, dichloromethane and dimethylformamide, ata temperature between 50° C. to 150° C.

The afore mentioned reactions involving the synthesis of the4,5-dihydro-pyrazole ring or the reaction of a compound comprising saidring are preferably carried out under an inert atmosphere, preferablyunder a nitrogen or argon atmosphere, to avoid oxidation of thering-system.

During some synthetic reactions described above the protection ofsensitive or reactive groups may be necessary and/or desirable. This canbe performed by using conventional protective groups like thosedescribed in Protective groups in Organic Chemistry, ed. J. F. W.McOmie, Plenum Press, 1973; T. W. Greene & P. G. M. Wuts and ProtectiveGroups in Organic Chemistry, John Wiley & sons, 1991. The respectiveparts of the description is hereby incorporated by reference and formspart of the disclosure. The protective groups may be eliminated whenconvenient by means well-known to those skilled in the art.

If the 4-substituted pyrazoline compounds of general formula I areobtained in form of a mixture of stereoisomers, particularly enantiomersor diastereomers, said mixtures may be separated by standard proceduresknown to those skilled in the art, e.g. chromatographic methods orcrystallization with chiral reagents. It is also possible to obtain purestereoisomers via stereoselective synthesis.

In a further aspect the present invention also provides a process forthe preparation of salts of 4-substituted pyrazoline compounds ofgeneral formula I and stereoisomers thereof, wherein at least onecompound of general formula I having at least one basic group is reactedwith at least one inorganic and/or organic acid, preferably in thepresence of a suitable reaction medium. Suitable reaction media include,for example, any of the ones given above. Suitable inorganic-acidsinclude hydrochloric acid, hydrobromic acid, phosphoric acid, sulfuricacid, nitric acid, suitable organic acids are e.g. citric acid, maleicacid, fumaric acid, tartaric acid, or derivatives thereof,p-toluenesulfonic acid, methanesulfonic acid or camphersulfonic acid.

In yet a further aspect the present invention also provides a processfor the preparation of salts of 4-substituted pyrazoline compounds ofgeneral formula I or stereoisomers thereof, wherein at least onecompound of general formula I having at least one acidic group isreacted with one or more suitable bases, preferably in the presence of asuitable reaction medium. Suitable bases are e.g. hydroxides, carbonatesor alkoxides, which include suitable cations, derived e.g. from alkalinemetals, alkaline earth metals or organic cations, e.g. [NH_(n)R_(4-n)]⁺,wherein n is 0, 1, 2, 3 or 4 and R represents a branched or unbranchedC₁₋₄-alkyl-radical. Suitable reaction media are, for example, any of theones given above.

In the presence of several acidic or basic groups, mono- or poly-saltsmay be formed. Compounds of the formula I having an acidic group, forexample a free carboxyl group, and a basic group, for example an aminogroup, may also be present in the form of inner salts, i.e., inzwitterionic form, or a part of the molecule may be present in the formof an inner salt and another part in the form of a normal salt.

Solvates, preferably hydrates, of the 4-substituted pyrazoline compoundsof general formula I, of corresponding stereoisomers, of correspondingN-oxides or of corresponding salts thereof may also be obtained bystandard procedures known to those skilled in the art.

4-Substituted pyrazoline compounds of general formula I, which comprisenitrogen-atom containing saturated, unsaturated or aromatic rings mayalso be obtained in the form of their N-oxides by methods well known tothose skilled in the art.

The purification and isolation of the inventive 4-substituted pyrazolinecompounds of general formula I, of a corresponding stereoisomer, orsalt, or N-oxide, or solvate or any intermediate thereof may, ifrequired, be carried out by conventional methods known to those skilledin the art, e.g. chromatographic methods or recrystallization.

The compounds of general formula I given above may also act as prodrugs,i.e. they represent a drug precusor, which following administration to apatient releases a drug in vivo via some kind of chemical and/orphysiological process (e.g., a prodrug on being brought to aphysiological pH and/or through an enzyme action is converted to adesired drug form; see, e.g., R. B. Silverman, 1992, “The OrganicChemistry of Drug Design and Drug Action”, Academic Press, Chp. 8). Inparticular, the compounds of general formula I give rise to a compoundof general formula I, wherein R³ represents a —OH moiety, uponadministration to a patient.

Prodrugs can be used to alter the biodistribution (e.g., to allowcompounds which would not typically enter the reactive site of theprotease) or the pharmacokinetics for a particular compound. Forexample, a hydroxyl group, can be esterified, e.g., with a carboxylicacid group to yield an ester. When the ester is administered to asubject, the ester is cleaved, enzymatically or non-enzymatically,reductively or hydrolytically, to reveal the hydroxyl group.

The 4-substituted pyrazoline compounds of general formula I given above,their stereoisomers, corresponding N-oxides, corresponding salts thereofand corresponding solvates are toxicologically acceptable and aretherefore suitable as pharmaceutical active substances for thepreparation of medicaments.

It has been found that the 4-substituted pyrazoline compounds of generalformula I given above, stereoisomers thereof, N-oxides thereof,corresponding salts and corresponding solvates have a high affinity tocannabinoid receptors, particularly cannabinoid 1 (CB₁)-receptors, i.e.they are selective ligands for the CB₁-receptor and act as modulators,e.g. antagonists, inverse agonists or agonists, on these receptors. Inparticular, these pyrazoline compounds show little or no development oftolerance during treatment, particularly with respect to food intake,i.e. if the treatment is interrupted for a given period of time aridthen continued afterwards, the inventively used pyrazoline compoundswill again show the desired effect. After ending the treatment with thepyrazoline compounds, the positive influence on the body weight is foundto continue.

Furthermore, these 4-substituted pyrazoline compounds show relativelyweak Herg channel affinity, thus a low risk of prolongation of theQT-interval is to be expected for these compounds.

In summary, the inventively used 4-subsituted pyrazoline compounds aredistinguished by a broad spectrum of beneficial effects, while at thesame time showing relatively little undesired effects, i.e. effectswhich do not positively contribute to or even interfere with the wellbeing of the patient.

Thus, an other aspect of the present invention relates to a medicamentcomprising at least one 4-substituted pyrazoline compound of generalformula I including the aforementioned excluded compounds, optionally inform of one of its stereoisomers, preferably enantiomers ordiastereomers, a racemate or in form of a mixture of at least two of itsstereoisomers, preferably enantiomers and/or diastereomers, in anymixing ratio, or a corresponding N-oxide thereof, or a physiologicallyacceptable salt thereof, or a corresponding solvate thereof, andoptionally at least one physiologically acceptable auxiliary agent.

Preferably said medicament is suitable for the modulation (regulation)of cannabinoid-receptors, preferably cannabinoid 1 (CB₁) receptors, forthe prophylaxis and/or treatment of disorders of the central nervoussystem, disorders of the immune system, disorders of the cardiovascularsystem, disorders of the endocrinous system, disorders of therespiratory system, disorders of the gastrointestinal tract orreproductive disorders.

Particularly preferably said medicament is suitable for the prophylaxisand/or treatment of psychosis.

Also particularly preferably said medicament is suitable for theprophylaxis and/or treatment of food intake disorders, preferablybulimia, anorexia, cachexia, obesity and/or type II diabetus mellitus(non-insuline dependent diabetes mellitus), more preferably obesity. Theinventive medicament also seems to be active in the prophylaxis and/ortreatment of appetency disorders, e.g. the pyrazoline compounds ofgeneral formula I also reduce the desire for sweets.

Also particularly preferably said medicament is suitable for theprophylaxis and/or treatment of cancer, preferably for the prophylaxisand/or treatment of one or more types of cancer selected from the groupconsisting of brain cancer, bone cancer, lip cancer, mouth cancer,esophageal cancer, stomach cancer, liver cancer, bladder cancer,pancreas cancer, ovary cancer, cervical cancer, lung cancer, breastcancer, skin cancer, colon cancer, bowel cancer and prostate cancer,more preferably for the prophylaxis and/or treatment of one or moretypes of cancer selected from the group consisting of colon cancer,bowel cancer and prostate cancer.

Particularly preferably said medicament is suitable for the prophylaxisand/or treatment of alcohol abuse and/or alcohol addiction, nicotineabuse and/or nicotine addiction, drug abuse and/or drug addiction and/ormedicament abuse and/or medicament addiction, preferably drug abuseand/or drug addiction and/or nicotine abuse and/or nicotine addiction.

Thus the inventive medicament is active in the treatment of abstinence,craving reduction and relapse prevention of alcohol intake. Theinventive medicament can also be used in the prophylaxis and/ortreatment of smoking addiction, cessation and/or dependence includingtreatment for craving reduction and relapse prevention of tobaccosmoking.

Medicaments and/or drugs, which are frequently the subject of misuseinclude opioids, barbiturates, cannabis, cocaine, amphetamines,phencyclidine, hallucinogens and benzodiazepines.

The medicament is also suitable for the prophylaxis and/or treatment ofone or more disorders selected from the group consisting of bonedisorders, preferably osteoporosis (e.g. osteoporosis associated with agenetic predisposition, sex hormone deficiency, or ageing),cancer-associated bone disease or Paget's disease of bone;schizophrenia, anxiety, depression, epilepsy, neurodegenerativedisorders, cerebellar disorders, spinocerebellar disorders, cognitivedisorders, cranial trauma, head trauma, stroke, panic attacks,peripheric neuropathy, inflammation, glaucoma, migraine, MorbusParkinson, Morbus Huntington, Morbus Alzheimer, Raynaud's disease,tremblement disorders, compulsive disorders, senile dementia, thymicdisorders, tardive dyskinesia, bipolar disorders, medicament-inducedmovement disorders, dystonia, endotoxemic shock, hemorrhagic shock,hypotension, insomnia, immunologic disorders, sclerotic plaques,vomiting, diarrhea, asthma, memory disorders, pruritus, pain, or forpotentiation of the analgesic effect of narcotic and non-narcoticanalgesics, or for influencing intestinal transit.

The medicament is also suitable for the prophylaxis and/or treatment ofone or more disorders selected from the group consisting of dementia andrelated disorders, preferably for the prophylaxis and/or treatment ofone or more types of dementia selected from the group consisting ofmemory loss, vascular dementia, mild cognitive impairment,frontotemporal dementia and Pick's disease; binge eating disorders;juvenile obesity; drug induced obesity; atypical depression; behaviouraladdictions; attention deficit disorders; Tourette's syndrome;suppression of reward-related behaviours; e.g. conditioned placeavoidance such as suppression of cocaine- and morphine inducedconditioned place preference; impulsivity; sexual dysfunction;preferably for the prophylaxis and/or treatment of one or more types ofsexual dysfunction selected from the group consisting of erectiledifficulty and female sexual dysfunction; seizure disorders; nausea;emesis; neuroinflammatory disease, preferably for the prophylaxis and/ortreatment of one or more types of neuroinflammatory diseases selectedfrom the group consisting of multiple sclerosis, demyelinisation relateddisorders, Guillan-Barré syndrome, viral encephalitis andcerebrovascular accidents; neurological disorders; muscle spasticity;traumatic brain injury; spinal cord injury; inflammation andimmunomodulatory disorders, preferably for the treatment and/orprophylaxis of one or more types of inflammation and immunomodulatorydisorders selected from the group consisting of cutaneous T-celllymphoma, rheumatoid arthritis, systemic lupus erythematosus, sepsis,sarcoidosis, idiopathic pulmonary fibrosis, bronchopulmonary dysplasia,retinal disease, scleroderma, renal ischemia, mycocardial infarction,cerebral ischemia, nephritis, hepatitis, glomerulonephritis, cryptogenicfibrosing aveolitis, psoriasis, transplant rejection, atopic dermatitis,vasculitis, allergy, seasonal allergic rhinitis, Crohn's disease,inflammatory bowel disease, reversible airway obstruction, adultrespiratory distress syndrome, chronic obstructive pulmonary disease andbronchitis; cerebral apoplexy; craniocerebral trauma; neuropathic paindisorders; gastric ulcers; atheriosclerosis and liver cirrhosis.

Another aspect of the present invention is the use of at least one4-substituted pyrazoline compound of general formula I given above assuitable active substances, optionally in form of one of thestereoisomers, preferably enantiomers or diastereomers, a racemate or inform of a mixture of at least two of the stereoisomers, preferablyenantiomers and/or diastereomers, in any mixing ratio, or acorresponding N-oxide thereof, or a corresponding salt thereof, or acorresponding solvate thereof, and optionally one or morepharmaceutically acceptable excipients, for the preparation of amedicament for the modulation of cannabinoid-receptors, preferablycannabinoid 1 (CB₁) receptors, for the prophylaxis and/or treatment ofdisorders of the central nervous system, disorders of the immune system,disorders of the cardiovascular system, disorders of the endocrinoussystem, disorders of the respiratory system, disorders of thegastrointestinal tract or reproductive disorders.

Particularly preferred is the use of at least one of the respective4-substituted pyrazoline compounds, optionally in form of one of thestereoisomers, preferably enantiomers or diastereomers, a racemate or inform of a mixture of at least two of the stereoisomers, preferablyenantiomers and/or diastereomers, in any mixing ratio, or acorresponding N-oxide thereof, or a corresponding salt thereof, or acorresponding solvate thereof, and optionally one or morepharmaceutically acceptable excipients, for the preparation of amedicament for the prophylaxis and/or treatment of psychosis.

Also particularly preferred is the use of at least one of the respective4-substituted pyrazoline compounds, optionally in form of one of thestereoisomers, preferably enantiomers or diastereomers, a racemate or inform of a mixture of at least two of the stereoisomers, preferablyenantiomers and/or diastereomers, in any mixing ratio, or acorresponding N-oxide thereof, or a corresponding salt thereof, or acorresponding solvate thereof, and optionally one or morepharmaceutically acceptable excipients, for the preparation of amedicament for the prophylaxis and/or treatment of food intakedisorders, preferably bulimia, anorexia, cachexia, obesity and/or typeII diabetus mellitus (non-insuline dependent diabetes mellitus), morepreferably obesity.

Also particularly preferred is the use of at least one of the pyrazolinecompounds as defined herein and optionally one or more pharmaceuticallyacceptable excipients, for the preparation of a medicament for thetreatment of metabolic syndrome.

The metabolic syndrome and definitions thereof are described in detailby Eckel et al., The Lancet, Vol. 365 (2005), 1415-1428, includedherewith by reference. One of the respective definitions was establishedby the WHO in 1998 (as described in Alberti et al., Diabet. Med. 1998,15, pages 539-53, the respective description thereof is herewithincorporated by reference and forms part of the present disclosure). Theother, more widely accepted, definition of the metabolic syndrome wasestablished by the Adult Treatment Panel (ATP III) of the US NationalCholesterol Education Program (NCEP) in 2001, as described in JAMA 2001;285; 2486-97, the respective description thereof is herewithincorporated by reference and forms part of the present disclosure.

The metabolic syndrome is characterized by an interaction of severalphysiological parameters such as triglycerides, lipids, blood pressure,glucose levels and insuline levels.

Even though obesity may play a critical role in the development ofmetabolic syndrome, many of its aspects are weight independent,especially some lipid parameters. Especially the positive influence onthe weight independent aspects of the metabolic syndrome (see e.g.Pagotto and Pasquali, The Lancet, Vol. 365 (2005), 1363, 1364, includedherewith by reference) like some blood parameters, especially lipidparameters is one of the major and surprising advantages of theinventively used substituted pyrazoline compounds.

Another aspect of the invention is the use of one or more pyrazolinecompounds as defined herein for the manufacture of a medicament forimprovement of cardiovascular and/or metabolic risk factors, such as oneor more of the following factors:

-   Elevated triglycerides, whereby elevated levels of triglycerides are    preferably understood as being >150 mg/dl,-   Low HDL cholesterol, whereby low levels of HDL cholesterol are    preferably understood as being <40 mg/dl in men and <50 mg/dl in    women,-   Hypertension, whereby Hypertension is preferably understood as    being >130/85 mmHg,-   Impaired fasting glucose, whereby impaired fasting glucose levels    are preferably understood as being >110 mg/dl,-   Insulin resistance-   Dyslipidemia.

Another aspect of the invention is the use of one or more pyrazolinecompounds as defined herein for the manufacture of a medicament for thetreatment of the weight independent aspects of metabolic syndrome.

Another aspect of the invention is a method for improving cardiovascularand/or metabolic risk factors, such as one or more of the followingfactors:

-   Elevated triglycerides, whereby elevated levels of triglycerides are    preferably understood as being >150 mg/dl,-   Low HDL cholesterol, whereby low levels of HDL cholesterol are    preferably understood as being <40 mg/dl in men and <50 mg/dl in    women,-   Hypertension, whereby hypertension is preferably understood as    being >130/85 mmHg,-   Impaired fasting glucose, whereby impaired fasting glucose levels    are preferably understood as being >110 mg/dl,-   Insulin resistance-   Dyslipidemia,-   in a subject, preferably a human.

Another aspect of the invention is a method for treating of the weightindependent aspects of metabolic syndrome.

Also particularly preferred is the use of at least one of the respective4-substituted pyrazoline compounds, optionally in form of one of thestereoisomers, preferably enantiomers or diastereomers, a racemate or inform of a mixture of at least two of the stereoisomers, preferablyenantiomers and/or diastereomers, in any mixing ratio, or acorresponding N-oxide thereof, or a corresponding salt thereof, or acorresponding solvate thereof, and optionally one or morepharmaceutically acceptable excipients, for the preparation of amedicament for the prophylaxis and/or treatment of cancer, preferablyfor the prophylaxis and/or treatment of one or more types of cancerselected from the group consisting of brain cancer, bone cancer, lipcancer, mouth cancer, esophageal cancer, stomach cancer, liver cancer,bladder cancer, pancreas cancer, ovary cancer, cervical cancer, lungcancer, breast cancer, skin cancer, colon cancer, bowel cancer andprostate cancer, more preferably for the prophylaxis and/or treatment ofone or more types of cancer selected from the group consisting of coloncancer, bowel cancer and prostate cancer.

Also particularly preferred is the use of at least one of the respective4-substituted pyrazoline compounds, optionally in form of one of thestereoisomers, preferably enantiomers or diastereomers, a racemate or inform of a mixture of at least two of the stereoisomers, preferablyenantiomers and/or diastereomers, in any mixing ratio, or acorresponding N-oxide thereof, or a corresponding salt thereof, or acorresponding solvate thereof, and optionally one or morepharmaceutically acceptable excipients, for the preparation of amedicament for the prophylaxis and/or treatment of alcohol abuse and/oralcohol addiction, nicotine abuse and/or nicotine addiction, drug abuseand/or drug addiction and/or medicament abuse and/or medicamentaddiction, preferably drug abuse and/or drug addiction and/or nicotineabuse and/or nicotine addiction.

Also particularly preferred is the use of at least one of the of therespective 4-substituted pyrazoline compounds, optionally in form of oneof the stereoisomers, preferably enantiomers or diastereomers, aracemate or in form of a mixture of at least two of the stereoisomers,preferably enantiomers and/or diastereomers, in any mixing ratio, or acorresponding solvate thereof, and optionally one or morepharmaceutically acceptable excipients, for the preparation of amedicament for the prophylaxis and/or treatment of one or more disordersselected from the group consisting of dementia and related disorders,preferably for the prophylaxis and/or treatment of one or more types ofdementia selected from the group consisting of memory loss, vasculardementia, mild cognitive impairment, frontotemporal dementia and Pick'sdisease; binge eating disorders; juvenile obesity; drug induced obesity;atypical depression; behavioural addictions; attention deficitdisorders; Tourette's syndrome; suppression of reward-relatedbehaviours; e.g. conditioned place avoidance such as suppression ofcocaine- and morphine induced conditioned place preference; impulsivity;sexual dysfunction; preferably for the prophylaxis and/or treatment ofone or more types of sexual dysfunction selected from the groupconsisting of erectile difficulty and female sexual dysfunction; seizuredisorders; nausea; emesis; neuroinflammatory disease, preferably for theprophylaxis and/or treatment of one or more types of neuroinflammatorydiseases selected from the group consisting of multiple sclerosis,demyelinisation related disorders, Guillan-Barré syndrome, viralencephalitis and cerebrovascular accidents; neurological disorders;muscle spasticity; traumatic brain injury; spinal cord injury;inflammation and immunomodulatory disorders, preferably for thetreatment and/or prophylaxis of one or more types of inflammation andimmunomodulatory disorders selected from the group consisting ofcutaneous T-cell lymphoma, rheumatoid arthritis, systemic lupuserythematosus, sepsis, sarcoidosis, idiopathic pulmonary fibrosis,bronchopulmonary dysplasia, retinal disease, scleroderma, renalischemia, mycocardial infarction, cerebral ischemia, nephritis,hepatitis, glomerulonephritis, cryptogenic fibrosing aveolitis,psoriasis, transplant rejection, atopic dermatitis, vasculitis, allergy,seasonal allergic rhinitis, Crohn's disease, inflammatory bowel disease,reversible airway obstruction, adult respiratory distress syndrome,chronic obstructive pulmonary disease and bronchitis; cerebral apoplexy;craniocerebral trauma; neuropathic pain disorders; gastric ulcers;atheriosclerosis and liver cirrhosis.

Medicaments/drugs, which are frequently the subject of misuse includeopioids, barbiturates, cannabis, cocaine, amphetamines, phencyclidine,hallucinogens and benzodiazepines.

Also preferred is the use of at least one of the respective4-substituted pyrazoline compounds, optionally in form of one of thestereoisomers, preferably enantiomers or diastereomers, a racemate or inform of a mixture of at least two of the stereoisomers, preferablyenantiomers and/or diastereomers, in any mixing ratio, or acorresponding N-oxide thereof, or a corresponding salt thereof, or acorresponding solvate thereof, and optionally one or morepharmaceutically acceptable excipients, for the preparation of amedicament for the prophylaxis and/or treatment of one or more disordersselected from the group consisting of bone disorders, preferablyosteoporosis (e.g. osteoporosis associated with a geneticpredisposition, sex hormone deficiency, or ageing), cancer-associatedbone disease or Paget's disease of bone; schizophrenia, anxiety,depression, epilepsy, neurodegenerative disorders, cerebella disorders,spinocerebellar disorders, cognitive disorders, cranial trauma, headtrauma, stroke, panic attacks, peripheric neuropathy, inflammation,glaucoma, migraine, Morbus Parkinson, Morbus Huntington, MorbusAlzheimer, Raynaud's disease, tremblement disorders, compulsivedisorders, senile dementia, thymic disorders, tardive dyskinesia,bipolar disorders, medicament-induced movement disorders, dystonia,endotoxemic shock, hemorrhagic shock, hypotension, insomnia, immunologicdisorders, sclerotic plaques, vomiting, diarrhea, asthma, memorydisorders, pruritus, pain, or for potentiation of the analgesic effectof narcotic and non-narcotic analgesics, or for influencing intestinaltransit.

Dementia is a disease characterized by the progressive deterioration incognitive and social adaptive functions that can eventually interferewith the patient's ability to live independently. Dementia alsoconstitutes of impairment in short- and long-term memory plus additionalsymptoms, such as problems with abstract thinking, judgment, orpersonality. An estimated 18 million patients suffer from dementiaworldwide. The most common forms of dementia include Alzheimer's diseaseand vascular dementia. Other forms are frontotemporal dementia andPick's disease.

Dementia can also be of vascular origin. Vascular dementia(atherosclerotic cerebrovascular disease) is considered to be the secondmost common dementia of. late life, affecting approximately 10-15% ofall cases. AD and vascular dementia can exist in isolation or together(mixed dementia). In vascular dementia, atherosclerotic changes incerebral vessels can lead to reduced local blood flow that results inmultiple small strokes (multi-infarct dementia). Vascular dementia ispharmacologically treated by stroke prophylaxis, and by treatment of thecognitive deficit.

Alzheimer's disease (AD), the most common and important form ofdementia, is a neurodegenerative disorder that is characterized byprogressive impairment of. cognitive functions, such as abstractreasoning and memory. Currently, an estimated 2 million people in theUnited States and 12 million worldwide are afflicted by this disease.Due to increasing life expectancy, it is predicted that there will beover 100 million AD patients worldwide by the year 2050. AD is one ofthe most prevalent illnesses in the elderly. The majority of AD patientsare in their sixties or older. More than 5% of all persons over the ageof 70 have significant memory loss due to AD.

AD is mainly characterized through a gradual development offorgetfulness. In further advanced disease stages, other failures incerebral function become increasingly apparent. This includes impairmentof speech, writing, and arithmetic skills. Visiospacial orientation,such as parking the car, dressing properly, and giving and understandingdirections to a location, can become defective or impaired. In latestage disease, patients forget how to use common objects and tools whileretaining necessary motor power and co-ordination for these activities.

Schizophrenia is characterized by profound disruption in cognition andemotion, affecting the most fundamental human attributes: language,thought, perception, affect, and sense of self. Positive symptomsinclude psychotic manifestations, such as hearing internal voices orexperiencing other sensations not connected to an obvious source(hallucinations) and assigning unusual significance or meaning to normalevents or holding fixed false personal beliefs (delusions). Negativesymptoms are characterized by affective flattening and lack ofinitiative or goals (avolition), loss of usual interests or pleasures(anhedonia), disturbances of sleep and eating, dysphoric mood(depressed, anxious, irritable, or angry mood) and difficultyconcentrating or focusing attention.

Major depression is a multifaceted disorder characterized by primarilyby dysphoric mood and loss of interest or pleasure in activities thatwere once enjoyable. Other physical and psychological symptoms includeinability to concentrate, motor disturbances (psychomotor retardation oragitation), feelings of worthlessness, inappropriate guilt, thoughts ofsuicide, and disturbances in appetite and sleep.

Anxiety disorders are a group of syndromes that include generalizedanxiety disorder, panic disorder, phobias, obsessive-compulsivedisorder, and post traumatic stress disorder. Although each disorder hasits own distinct features, all share common symptoms of excessiveworrying, intense fears and dread, hypervigilance and/or somaticsymptoms, in the absence of a dangerous situation.

Normal sexual function requires, among others, the ability to achieveand maintain penile erection. Major anatomic structures of the penisthat are involved in erectile function include the corpus cavernosum,corpus spinosum, and the tunica albuginea (a collagenous sheath thatsurrounds each corpus). The corpora are composed of a mass of smoothmuscle (trabecula) which contains a network of endothelial-lined vessels(lacunar spaces). Penile tumescence and erection is caused by relaxationof the arteries and corporal smooth muscles, while closing emissaryveins, leading to increased blood flow into the lacunar network. Centraland peripheral innervation contributes to regulation of the erectileresponse.

Erectile dysfunction (ED) may result from failure to initiate, fill, orstore adequate blood volume within the lacunar network of the penis.Depending on the underlying dysfunction, ED may be vasculogenic,neurogenic, endocrinologic, diabetic, psychogenic, ormedication-related.

ED affects 10-25% of middle-aged and elderly men, and has a profoundimpact on the well-being of affected men. It is currently treated usingPDE5 inhibitors such as vardenafil, tadalifil, and sildenafil.Intraurethral alpostadil (prostaglandin El) may be used in patients thatfail on oral agents. In addition, vacuum constriction devices (VCD) area well-established, noninvasive therapy.

Female sexual dysfunction (FSD) is highly prevalent, age-related, andprogressive. It affects 30 to 50% of women. FSD denotes a range ofmedical problems and is categorized according to disorders of (1)desire, (2) arousal, (3) orgasm and (4) sexual pain, and symptomsinclude diminished vaginal lubrication, pain and discomfort withintercourse, decreased arousal, and difficulty achieving orgasm. On amolecular level, vasoactive intestinal peptide (VIP), nitic oxide (NO),and sex hormones such as estrogens and androgens have been suggested tobe important in female sexual function. Current treatment approachesinclude estrogen replacement therapy, methyl testosterone, PDE5inhibitors such as sildenafil, the NO-donor L-arginine, prostaglandinEl, phentolamine, and the dopamine agonists apomorphine.

The medicament according to the present invention may be in any formsuitable for the application to humans and/or animals, preferably humansincluding infants, children and adults and can be produced by standardprocedures known to those skilled in the art. The medicament can beproduced by standard procedures known to those skilled in the art, e.g.from the table of contents of “Pharmaceutics: The Science of DosageForms”, Second Edition, Aulton, M. E. (ED. Churchill Livingstone,Edinburgh (2002); “Encyclopedia of Pharmaceutical Technology”, SecondEdition, Swarbrick, J. and Boylan J. C. (Eds.), Marcel Dekker, Inc. NewYork (2002); “Modern Pharmaceutics”, Fourth Edition, Banker G. S. andRhodes C. T. (Eds.) Marcel Dekker, Inc. New York 2002 y “The Theory andPractice of Industrial Pharmacy”, Lachman L., Lieberman H. And Kanig J.(Eds.), Lea & Febiger, Philadelphia (1986). The respective descriptionsare hereby incorporated by reference and form part of the disclosure.The composition of the medicament may vary depending on the route ofadministration.

The medicament of the present invention may for example be administeredparentally in combination with conventional injectable liquid carriers,such as water or suitable alcohols. Conventional pharmaceuticalexcipients for injection, such as stabilising agents, solubilizingagents, and buffers, may be included in such injectable compositions.These medicaments may for example be injected intramuscularly,intraperitoneally, or intravenously.

Medicaments according to the present invention may also be formulatedinto orally administrable compositions containing one or morephysiologically compatible carriers or excipients, in solid or liquidform. These compositions may contain conventional ingredients such asbinding agents, fillers, lubricants, and acceptable wetting agents. Thecompositions may take any convenient form, such as tablets, pellets,granules, capsules, lozenges, aqueous or oily solutions, suspensions,emulsions, or dry powdered forms suitable for reconstitution with wateror other suitable liquid medium before use, for immediate or retardedrelease. The multiparticulate forms, such as pellets or granules, maye.g. be filled into a capsule, compressed into tablets or suspended in asuitable liquid.

Suitable controlled release formulations, materials and methods fortheir preparation are known from the prior art, e.g. from the table ofcontents of “Modified-Release Drug Delivery Technology”, Rathbone, M. J.Hadgraft, J. and Roberts, M. S. (Eds.), Marcel Dekker, Inc., New York(2002); “Handbook of Pharmaceutical Controlled Release Technology”,Wise, D. L. (Ed.), Marcel Dekker, Inc. New York, (2000); “ControlledDrug Delivery”, Vol, I, Basic Concepts, Bruck, S. D. (Ed.), CRD PressInc., Boca Raton (1983) y de Takada, K. and Yoshikawa, H., “Oral DrugDelivery”, Encyclopedia of Controlled Drug Delivery, Mathiowitz, E.(Ed.), John Wiley & Sons, Inc., New York (1999), Vol. 2, 728-742; Fix,J., “Oral drug delivery, small intestine and colon”, Encyclopedia ofControlled Drug Delivery, Mathiowitz, E. (Ed.), John Wiley & Sons, Inc.,New York (1999), Vol. 2, 698-728. The respective descriptions are herebyincorporated by reference and form part of the disclosure.

Medicaments according to the present invention may also comprise anenteric coating, so that their dissolution is dependent on pH-value. Dueto said coating the medicament can pass the stomach undissolved and therespective 4-substituted pyrazoline compound of general formula I isliberated in the intestinal tract. Preferably the enteric coating issoluble at a pH value of 5 to 7.5. Suitable materials and methods forthe preparation are known from the prior art.

Typically, the medicaments according to the present invention maycontain 1-60% by weight of one or more 4-substituted pyrazolinecompounds as defined herein and 40-99 % by weight of one or moreauxiliary substances (additives).

The liquid oral forms for administration may also contain certainadditives such as sweeteners, flavoring, preservatives, and emulsifyingagents. Non-aqueous liquid compositions for oral administration may alsobe formulated, containing edible oils. Such liquid compositions may beconveniently encapsulated in e.g., gelatin capsules in a unit dosageamount.

The compositions of the present invention may also be administeredtopically or via a suppository.

The daily dosage for humans and animals may vary depending on factorsthat have their basis in the respective species or other factors, suchas age, sex, weight or degree of illness and so forth. The daily dosagefor humans may preferably be in the range from 1 to 2000, preferably 1to 1500, more preferably 1 to 1000, even more preferably 1 to 150milligrams of active substance to be administered during one or severalintakes per day.

Pharmacological Methods

I. In-vitro Determination of Affinity to CB1/CB2-Receptors

a)

The in-vitro determination of the affinity of the inventive4-substituted pyrazoline compounds to CB₁/CB₂-Rezeptors is carried outas described in the publication of Ruth A. Ross, Heather C. Brockie etal., “Agonist-inverse agonist characterisation at CB₁ and CB₂cannabinoid receptors of L-759633, L759656 and AM630”, British Journalof Pharmacology, 126, 665-672, (1999), whereby the transfected human CB₁and CB₂ receptors of Receptor Biology, Inc. are used. The radioligandused for both receptors is [³H]-CP55940. The respective parts of thedescription is hereby incorporated by reference and forms part of thepresent disclosure.

b)

Rat Cerebellum CB1 Binding

Binding affinity to CB1 receptor was evaluated according to amodification of the method described by Govaerts et al., Eur J PharmacSci 23, 233-243 (2004). The respective parts of the description ishereby incorporated by reference and forms part of the presentdisclosure.

Briefly, cerebellum from male wistar rats (250-300 g) were carefullydissected on ice and homogenates were prepared with Potter-Helveheim ina cold 50 mM Tris-HCl solution containing 5 mM MgCl₂, 1 mM EDTA and 0.25M sucrose, pH 7.4. The suspension was centrifuged at 1,00×g for 5minutes. The supernatants were collected and centrifuged 50,000×g for 15minutes. The resulting pellets were then resuspended in Tris-HCl bufferwithout sucrose, homogenized and incubated for 15 min at 37° C. in anorbital shaker bath and centrifuged again at 50,000×g for 15 min.Pellets were weighted, resuspended in Tris-HCl buffer without sucrose,homogenized with Ultraturrax at 13,500 rpm for 3×5 seconds and alicuotedin 0.9 ml volumes in Eppendorf tubes. Alicuotes were centrifuged at20,800×g for 5 minutes, supernatants discarded and pellets were frozenat −80° C. until use. Total protein concentration was determined usingthe Bio-Rad Lowry method based kit. Competitive binding experiments wereperformed in presence of 1 nM [³H]-CP 55,940 in siliconized glass tubescontaining 100 μg protein/tube resuspended in 1 ml final volume of 50 mMTris-HCl, 5 mM MgCl₂, 1 mM EDTA, 0.5% (w/v) bovine serum albumin, pH7.4. Compounds were present at various concentrations and the nonspecific binding was determined in the presence of 10 μM HU-210. After 1hour incubation at 30° C., the suspension was rapidly filtered through0.5% PEI pre-treated GF/B fiber filters on a 96-well harvester andwashed 3 times with 3 ml ice-cold binding buffer without bovine serumalbumin. Radioactivity on filters was measured with Wallac Winspectral1414 counter by liquid scintillation in 6 ml Ecoscint H (NationalDiagnostics, U.K.). Assays were made in triplicates.

Binding data were analyzed by non-linear regression with the softwareGraphPad Prism Version 3.03.

II. In-vivo Bioassay System for Determination of Cannabinoid Activity

Mouse Tetrad Model

Substances with affinity for cannabinoid receptors are known to producea wide range of pharmacological effects. It is also known thatintravenous administration of a substance with affinity for cannabinoidreceptors in mice produces analgesia, hypothermia, sedation andcatalepsy. Individually, none of these effects can be considered asproof that a tested substance has affinity for cannabinoid-receptors,since all of these effects are common for various classes of centrallyactive agents. However, substances, which show all of these effects,i.e. substances that are active in this so-called tetrad model areconsidered to have affinity for the cannabinoid receptors. It hasfurther been shown that cannabinoid receptor antagonists are highlyeffective in blocking the effects of a cannabinoid agonist in the mousetetrad model.

The tetrad model is described, for example, in the publication of A. C.Howlett et al, International Union of Pharmacology XXVII. Classificationof Cannabinoid Receptors, Pharmacol Rev 54, 161-202, 2002 and David R.Compton et al., “In-vivo Characterization of a Specific CannabinoidReceptor Antagonist (SR141716A): Inhibition ofTetrahydrocannbinol-induced Responses and Apparent Agonist Activity”, J.Pharmacol. Exp. Ther. 277, 2, 586-594, 1996. The corresponding parts ofthe descriptions=are hereby incorporated by reference.

Material and Methods

Male NMRI mice with a weight of 20-30 g (Harlan, Barcelona, Spain) areused in all of the following experiments.

Before testing in the behavioural procedures given below, mice areacclimatised to the experimental setting. Pre-treatment control valuesare determined for analgesia hot plate latency (in seconds), rectaltemperature, sedation and catalepsy.

In order to determine the agonistic activity of the substance to betested, the mice are injected intravenously with the substance to betested or the vehicle alone. 15 minutes after injection, latency-in hotplate analgesia is measured. Rectal temperature, sedation and catalepsyare measured 20 minutes after injection.

In order to determine the antagonistic activity the identical procedureis used as for the determination of the agonistic effects, but with thedifference that the substance to be evaluated for its antagonisticactivity is injected 5 minutes before the intravenous injection of 1.25mg/kg Win-55,212 a known cannabinoid-receptor agonist.

Hot Plate Analgesia

The hot plate analgesia is determined according to the method describedin Woolfe D. et al. “The evaluation of analgesic action of pethidinehydrochloride (Demerol)”, J. Pharmacol. Exp. Ther. 80, 300-307,l944. Therespective description is hereby incorporated by reference and formspart of the present disclosure.

The mice are placed on a hot plate (Harvard Analgesimeter) at 55±0.5° C.until they show a painful sensation by licking their paws or jumping andthe time for these sensations to occur is recorded. This reading isconsidered the basal value (B). The maximum time limit the mice areallowed to remain on the hot plate in absence of any painful response is40 seconds in order to prevent skin damage. This period is called thecut-off time (PC).

Fifteen minutes after the administration of the substance to be tested,the mice are again placed on the hot plate and the afore describedprocedure is repeated. This period is called the post-treatment reading(PT).

The degree of analgesia is calculated from the formula:% MPE of Analgesia=(PT−B)/(PC−B)×100MPE=Maximum possible effect.Determination of Sedation and Ataxia

Sedation and ataxia is determined according to the method described inDesmet L. K. C. et al. “Anticonvulsive properties of Cinarizine andFlunarizine in Rats and Mice”, Arzneim.-Forsch. (Frug Res) 25, 9, 1975.The respective description is hereby incorporated by reference and formspart of the present disclosure.

The chosen scoring system is

-   0: no ataxia;-   1: doubtful;-   2: obvious calmness and quiet;-   3 pronounced ataxia;    prior to as well as after treatment.

The percentage of sedation is determined according to the formula:% of sedation=arithmetic mean/3×100Hypothermia:

Hypothermia is determined according to the method described in David R.Compton et al. “In-vivo Characterization of a Specific CannabinoidReceptor Antagonist (SR141716A) Inhibition ofTetrahydrocannbinol-induced Responses and Apparent Agonist Activity”, J.Pharmacol Exp Ther. 277, 2, 586-594, 1996. The respective description ishereby incorporated by reference and forms part of the presentdisclosure.

The base-line rectal temperatures are determined with a thermometer(Yello Springs Instruments Co., Panlabs) and a thermistor probe insertedto 25 mm before the administration of the substance to be tested. Rectaltemperature is again measured 20 minutes after the administration of thesubstances to be tested. The temperature difference is calculated foreach animal, whereby differences of ≧−2° C. are considered to representactivity.

Catalepsy:

Catalepsy is determined according to the method described in AlpermannH. G. et al. “Pharmacological effects of Hoe 249: A new potentialantidepressant” Drugs Dev. Res. 25, 267-282.1992. The respectivedescription is hereby incorporated by reference and forms part of thepresent disclosure.

The cataleptic effect of the substance to be tested is evaluatedaccording to the duration of catalepsy, whereby the animals are placedhead downwards with their kinlegs upon the top of the wooden block.

The chosen scoring system is:

Catalepsy for:

-   more than 60 seconds=6; 50-60 seconds=5, 40-50 seconds=4, 30-40    seconds=3, 20-30 seconds=2, 5-10 seconds=1, and less than 5    seconds=0.

The percentage of catalepsy is determined according to the followingformula:% Catalepsy=arithmetic mean/6×100III. In vivo Testing for Antiobesic Activitya) Accute Treatment

Normally handled rats were habituated to a reversed cycle 12/12 h, andthe tested compound as well as saline was acutely orally administered.After administration the cumulated food intake (g) was measured at 6 hand 24 h. Following that the difference in body weight between controland compound treated animals was measured. This is a variation of thetest according to Colombo et al. as described below.

b) Long-Term Treatment

The in-vivo testing for antiobesic activity of the inventive pyrazolinecompounds is carried out as described in the publication of G. Colomboet al., “Appetite Suppression and Weight Loss after the CannabinoidAntagonist SR 141716”; Life Sciences, 63 (8), 113-117, (1998). Therespective part of the description is hereby incorporated by referenceand forms part of the present disclosure.

IV. In vivo Testing for Antidepressant Activity

The in-vivo testing for antidepressant activity of the inventivepyrazoline compounds in the water despair test is carried out asdescribed in the publication of E. T. Tzavara et al., “The CB1 receptorantagonist SR141716A selectively increases monoaminergicneurotransmission in the medial prefrontal cortex: implications fortherapeutic actions”; Br. J. Pharmacol. 2003, 138(4):544:53. Therespective part of the description is hereby incorporated by referenceand forms part of the present disclosure.

The present invention is illustrated below with the aid of examples.These illustrations are given solely by way of example and do not limitthe general spirit of the present invention.

V. In vitro Determination of Antagonism to CB1-Receptor

Membrane Preparation:

Chinese hamster ovary (CHO) cells stably expressing recombinant humancannabinoid 1 receptor (CB1) were cultured in nutrient mixture Ham's F12 supplemented with 10% heat-inactivated fetal bovine serum, 2 mML-glutamine, 50 U/ml penicillin, 50 U/ml streptomycin and 0.5 mg/mlgeneticin. In order to obtain cells, culture flasks were washed twicewith phosphate buffered saline and scraped. Then, cells were collectedby centrifugation (200×g, 10 min) and stored dry at −80° C. Cells werehomogenized in ice-cold 20 mM HE PES, 10 mM EDTA (pH 7.5) andcentrifuged at 40,000×g for 15 min at 4° C. The pellet was resuspendedin 20 mM HEPES, 0.1 mM EDTA (pH 7.5) and centrifuged for 15 min at 4° C.The final pellet was resuspended in 20 mM HEPES, 0.1 mM EDTA (pH 7.5),and divided in aliquots and stored at −80° C. until use.

[³⁵S]GTPγS Binding Assay:

The reaction was performed in 96-well plates. Membranes (15 μgprotein/well) were incubated for 60 min at 30° C. in buffer (50 mM HEPES, 100 mM KCl, 5 mM MgCl₂, 1 mM EDTA, 0.1% wt/vol bovine serumalbumin, 5 μM GDP, saponin (10 μg/ml), 0.5 nM [³⁵S]GTPγS, pH 7.4) withcompound at 1 μM final concentration in either the absence or presenceof dose response curve of agonist WIN 55,212-2 between 3 nM and 3 μM.The incubation was terminated by rapid filtration through MilliporeMultiscreen glass fiber FB, and rinsed two-times with ice-cold assaybuffer. Filter plates were dried and 30 μl of scintillation liquid wasadded. Radioactivity was determined using Wallac Microbeta Trilux. Eachexperiment was performed at least in duplicate. A WIN 55,212-2dose-response either alone or in the presence of Rimonabant (1 μM) wassystematically performed.

Calculations:

The average of basal [35S]GTPγS binding was subtracted from all bindingdata. In order to compare the antagonism results from one screeningcampaign to another one, the difference between the maximal agonisteffect of WIN 55,212-2 alone, and the maximal antagonism effect due toWIN 55,212-2 plus Rimonabant (1 μM) was defined as 100%.

Further Methods:

Alcohol Intake

The following protocol may be used to evaluate the effects of alcoholintake in alcohol preferring (P) female rats (e.g. bred at IndianaUniversity) with an extensive drinking history. The following referenceprovides detailed a description of P rats: Lumeng, L, et al., “Differentsensitivities to ethanol in alcohol-preferring and-nonpreferring rats,”Pharmacol, Biochem Behav., 16, 125-130 (1982).

Female rats are given 2 hours of access to alcohol (10% v/v and water,2-bottle choice) daily at the onset of the dark cycle. The rats aremaintained on a reverse cycle to facilitate experimenter interactions.The animals are initially assigned to four groups equated for alcoholintakes: Group 1-vehicle; Group 2-positive control (e. g. 5.6 mg/kgAM251; Group 3-low dose test compound; and Group 4-high dose of testcompound. Test compounds are generally mixed into a vehicle of 30%(w/v)-cyclodextrin in distilled water at a volume of 1-2 ml/kg. Vehicleinjections are given to all groups for the first two days of theexperiment. This is followed by 2 days of drug injections (to theappropriate groups) and a final day of vehicle injections. On the druginjection days, drugs are given sc 30 minutes prior to a 2-hour alcoholaccess period. Alcohol intake for all animals is measured during thetest period and a comparison is made between drug and vehicle-treatedanimals to determine effects of the compounds on alcohol drinkingbehavior.

Additional drinking studies can be done utilizing female C57BI/6 mice(Charles River). Several studies have shown that this strain of micewill readily consume alcohol with little to no manipulation required(Middaugh et al., “Ethanol Consumption by C57BU6 Mice: Influence ofGender and Procedural Variables” Alcohol, 17 (3), 175-183, 1999; Le etal., “Alcohol Consumption by C57BL/6, BALA/c, and DBA/2 Mice in aLimited AccessParadigm” PharmacologyBiochemistry and Behavior, 47,375-378, 1994).

For example, upon arrival mice are individually housed and givenunlimited access to powdered rat chow, water and a 10% (w/v) alcoholsolution. After 2-3 weeks of unlimited access, water is restricted for20 hours and alcohol is restricted to only 2 hours access daily. This isdone in a manner that the access period was the last 2 hours of the darkpart of the light cycle.

Once drinking behavior is stabilized, testing can commence. Mice areconsidered stable when the average alcohol consumption for 3 days is 20%of the average for all 3 days. Day 1 of test consists of all micereceiving vehicle injection (sc or ip). Thirty to 120 minutes postinjection access is given to alcohol and water. Alcohol consumption forthat day is calculated (g/kg) and groups are assigned so that all groupshave equivocal alcohol intake. On day 2 and 3, mice are injected withvehicle or drug and the same protocol as the previous day is followed.Day 4 is wash out and no injections are given. Data is analyzed usingrepeated measures ANOVA. Change in water or alcohol consumption iscompared back to vehicle for each day of the test. Positive resultswould be interpreted as a compound that was able to significantly reducealcohol consumption while having no effect on water

Oxygen Consumption Methods:

Whole body oxygen consumption is measured using an indirect calorimeter(Oxymax from Columbus Instruments, Columbus, Ohio) in male SpragueDawley rats (if another rat strain or female rats are used, it will bespecified). Rats (e.g. 300-380 g body weight) are placed in thecalorimeter chambers and the chambers are placed in activity monitors.These studies are done during the light cycle. Prior to the measurementof oxygen consumption, the rats are fed standard chow ad libitum. Duringthe measurement of oxygen consumption, food is not available. Basalpre-dose oxygen consumption and ambulatory activity are measured every10 minutes for 2.5 to 3 hours. At the end of the basal pre-dosingperiod, the chambers are opened and the animals are administered asingle dose of compound (the usual dose range is 0.001 to 10 mg/lkg) byoral gavage (or other route of administration as specified, i. e., sc,ip, iv). Drugs are prepared in methylcellulose, water or other specifiedvehicle (examples include PEG400, 30% beta-cyclo dextran and propyleneglycol). Oxygen consumption and ambulatory activity are measured every10 minutes for an additional 1-6 hours post-dosing.

The Oxymax calorimeter software calculates the oxygen consumption(ml/kg/h) based on the flow rate of air through the chambers anddifference in oxygen content at inlet and output ports. The activitymonitors have 15 infrared light beams spaced one inch apart on eachaxis, ambulatory activity is recorded when two consecutive beams arebroken and the results are recorded as counts.

Resting oxygen consumption, during pre-and post-dosing, is calculated byaveraging the 10-min02 consumption values, excluding periods of highambulatory activity (ambulatory activity count>100) and excluding thefirst 5 values of the pre-dose period and the first value from thepost-dose period. Change in oxygen consumption is reported as percentand is calculated by dividing the post-dosing resting oxygen consumptionby the pre-dose oxygen consumption *100. Experiments will typically bedone with n=4-6 rats and results reported are mean +/−SEM.

Interpretation:

An increase in oxygen consumption of >10% is considered a positiveresult. Historically, vehicle-treated rats have no change in oxygenconsumption from pre-dose basal.

Nicotine Dependence

An intravenous nicotine self-administration model or place preferencemodel may be used to assess the effects of a test compound on nicotinedependence (see, e.g., Vastola, et al. Physiol. Behav. 77:107-114, 2002;Brower, et al., Brain Res. 930:12-20, 2002).

Place Preference

Sprague-Dawley rats are used in this study (Vastola, et al., 2002).Animals are housed in a temperature-controlled, 12 h/12 h illuminationcycle with ad libitum access to food and water. Conditioning and testingare conducted in a chamber divided into two compartments with a doorseparating the two compartments. Behavior of the animals is recorded byvideo camera.

Animals are habituated to the injection procedure for several days. Theanimals are then placed into the test chamber and given free access toboth compartments. The initial preference for a particular compartmentis determined. For the conditioning trials, animals are injected withnicotine and restricted to the nonpreferred compartment, or the animalsare injected with saline and restricted to the preferred compartment. Ontest day, the door separating the compartments is removed, the animal isplaced in the center of the chamber and allowed to move freely betweencompartments. Time spent in each compartment is scored. Preferentialoccupancy of the nicotine compartment follows from the conditionedreinforcing effects of nicotine.

Self-Administration

Self-administration in animals is a predictor of a compound's abusepotential in humans. Modifications to this procedure may also be used toidentify compounds that prevent or block the reinforcing properties ofdrags that have abuse potential. A compound that extinguishes theself-administration of a drag may prevent that drag's abuse or itsdependence.

Sprague-Dawley rats are used in this study. Initially, animals arehoused in a temperature- controlled, 12 h/12 h illumination cycle withad libitum access to food and water. The animals are then implanted withjugular catheters which exit through the animal's back, and each animalis placed in an individual operant chamber (Brower, et al., 2002). Thecatheters are connected to a computer-driven syringe pump which islocated outside of the chamber. The chamber contains two levers with agreen light located above each lever. The light is illuminated whennicotine is available.

In a self-administration test, animals are placed in the operantchambers and the levers are randomly designated as an active andinactive lever. Each response on the active lever produces an infusionof nicotine. Presses on the inactive lever have no effect, but are alsorecorded. Animals are then trained to self-administer nicotine over aset period of time by having drag access during each daily session.Illumination of the chamber house light signals the beginning of thesession and the availability of nicotine. When the session ends, thehouse light is turned off. Initially, a nicotine infusion occurs withevery press of the active lever. Once lever-pressing behavior has beenestablished, the number of presses to produce a nicotine infusion isincreased. After stable nicotine self-administration is obtained, theeffect of a test compound on the nicotine-reinforced behavior may beevaluated. Administration of this test compound prior to the session caneither potentiate, extinguish, or produce no change to theself-administrating behavior. Tests are conducted every two days, andthe order of the administration of the test compound doses iscontrolled.

Alzheimer/Dementia Experiments

Morris Water Maze Task

The Morris water maze is a behavioral in vivo test to measure spatialorientation learning and memory through a complex learning task. It ishighly suitable for testing compounds that enhance learning and memory.A circular water tank or pool (diameter 2 m, height 0.7 m) is filledwith water, and a 10 cm2 platform is placed 1-1.5 cm below the watersurface at a defined location within the pool. The-escape. platform isnot visible for an animal swimming in the water tank. For theexperiment, a rat or mouse is placed into the pool to swim freely.

The animals have the task to localize the submerged platform, and thetime and distance required for successful retrieval is measured.Multiple extra-maze cues are provided by the furniture in the room,including desks, computer equipment, a second water tank, the presenceof the experimenter, and by a radio on a shelf that is playing softly.

Before administration of the test compound, animals are usually trainedin the task 4 times a day for 5 days. Test compounds are administeredorally or intraperitoneally on the day of the experiment at a definedtime (e.g., 30 minutes before the first swim test). Control animals aredosed with the corresponding vehicle not containing test compound.Active compounds yield shorter times and distances to localize theplatform (i.e., the better the animal remembers the location of theplatform, the shorter the distance covered and the faster the platformis reached).

The test can also be carried out using transgenic or cognitivelyimpaired animals. Cognitive impairment is induced either by old age orexperimentally through brain lesions, such as bilateral lesions of the,entorhinal cortex in rats. Such lesions can be induced by intracerebralinjections of the excitotoxin ibotenic acid.

Object Recognition Task

The object recognition task is used to assess the effects of compoundson the cognitive performance of rodents. A rat is placed in an openfield, in which two identical objects are located. The rats inspectsboth objects during the initial trial of the test. After a certainretention interval (e.g., 24 hours), a second trial is carried out.Here, one of the two objects used in the first trial (the ‘familiar’object) and a novel object are placed in the open field, and theinspection time at each of the objects is measured. Good retention isreflected by higher exploration times towards the novel compared withthe ‘familiar’ object.

Administration of the putative cognition enhancer prior to the firsttrial predominantly allows assessment of the effects on acquisition, andon the consolidation processes. Administration of the test compoundafter the first trial allows to assess the effects on consolidationprocesses, whereas administration before the second trial allows tomeasure effects on retrieval processes.

Passive Avoidance Task

The passive avoidance task assesses memory performance in rats and mice.The inhibitory avoidance uses an apparatus consisting of a box with twocompartments separated by a guillotine door that can be operated by theexperimenter. One compartment is illuminated with bright light, and theother compartment is dark. A threshold of 2 cm separates the twocompartments when the guillotine door is 15 raised. When the door isopen, the illumination in the dark compartment is about 2 lux. The lightintensity is about 500 lux at the center of the floor of the lightcompartment.

Two habituation sessions, one shock session, and a retention session aregiven, separated by inter-session intervals of 24 hours. During thehabituation sessions and the retention session, the rat is allowed toexplore the apparatus for 300 seconds. The rat is placed in the lightcompartment, facing the wall opposite to the guillotine door. After anaccommodation period of 15 seconds, the guillotine door is opened sothat all parts of the apparatus can be visited freely. Rats normallyavoid brightly lit areas and will enter the dark compartment within afew seconds.

In the shock session, the guillotine door between the compartments islowered as soon as the rat has entered the dark compartment with allpaws, and a scrambled 1 mA footshock is administered for 2 seconds. Thenthe rat is removed from the apparatus and returned into its home cage.The procedure during the retention session is identical to that of thehabituation sessions.

The step-through latency, that is, the first latency of entering thedark compartment (in seconds) during the retention session is an indexof the memory performance of the animal: a better retention is assumedif the latency to enter the dark compartment is longer. A test compoundis given 30 minutes before the shock session, together with 1 mg/kgscopolamine. Scopolamine impairs the memory performance during theretention session 24 hours later. If the test compound increases theenter latency compared with the scopolamine-treated controls, it isconsidered to possess cognition enhancing activity. T-maze SpontaneousAlternation Task

The T-maze spontaneous alternation task (TeMCAT) assesses the spatialmemory performance in mice. The start arm and the two goal arms of theT-maze are provided with guillotine doors that can be operated manuallyby the experimenter. A mouse is put into the start arm at the beginningof training. In the first trial, either the left or right goal arm isblocked by lowering the respective guillotine door (forced trial).

After the mouse has been released from the start arm, it will explorethe maze, eventually entering the open goal arm, and return to the startposition, where it will be confined for 5 seconds, by lowering theguillotine door. Then, the animal can choose freely between the left andright goal arm (all guillotine-doors opened) during 14 additional trials(free choice trials). As soon as a mouse has entered one goal arm, theother arm is closed. The mouse eventually returns to the start arm andis free to visit whichever arm it wants after having been confined tothe start arm for 5 seconds. After completion of 14 free choice trialsin one session, the animal is removed from the maze.

Out of the 14 trials the alternations in percent are calculated. Thispercentage and the total time needed to complete the first forced trialand the subsequent 14 free choice trials (in seconds) is analyzed. Inaddition, cognitive deficits can be induced by injection of scopolamine30 minutes before the start of the training session. A cognitionenhancer, administered before the training session, will at leastpartially, antagonize the scopolamine-induced reduction in thespontaneous alternation rate.

Depression Model

A forced swim or tail suspension model may be used to assess theefficacy of antidepressant compounds (see, e.g., Porsolt, et al., Nature266:730-732, 1977; Stem, et al., Psychopharmacology 85:367-370, 1985).

Forced Swim Test

Rats or mice are placed in a cylinder filled with water 23-25° C. fromwhich no escape is possible. Initially, animals struggle and try toescape, but eventually adopt a characteristic immobile posture and makeno further attempts to escape except for small movements needed theirhead above water. Animals are dosed with a compound and the activity(swimming or climbing) or immobility is measured by an observer. Theimmobility is considered by some to reflect a ‘behavioral despair’ inwhich animals cease to struggle to escape the aversive situation. A widevariety of clinically used antidepressants (TCAs, MAOs, SSRIs,atypicals) decrease immobility in this test and has a good predictivevalidity in that it detects antidepressants with different mechanisms ofaction but its construct validity is weak. At least two distinct activebehavioral patterns are produced by pharmacologically selectiveantidepressant drugs. Serotonin-selective reuptake inhibitors increaseswimming behavior, whereas drugs acting primarily to increaseextracellular levels of norepinephrine or dopamine increase climbingbehavior. There are false positives (psychostimulants) but relativelyfew false negatives ([beta]-adrenergic agonists). The test is sensitiveto muscle-relaxant (benzodiazepines) and sedative (neuroleptics)effects, leading to enhanced immobility. False positives and falsenegatives can often be screened by measuring if the compound produceslocomotor stimulation or sedation.

Tail Suspension Test

When suspended by the tail, mice will initially struggle and try toescape and then alternate between active escape attempts and immobility.In this test, animals are dosed with a compound and the immobility ismeasured by an observer for 6 min.

Porsolt describes the immobile behavior as ‘behavioral despair’ whichanimals cease to struggle to escape the aversive situation. A largevariety of clinically antidepressants (tricyclics, MAOIs, SSRIs, andatypicals) reduce immobility in this model. The test has a goodpredictive validity for antidepressant activity and works for mostantidepressant classes including but has some false positives(psychostimulants). The test is sensitive to muscle-relaxant(benzodiazepines) and sedative (neuroleptics) effects, which lead toenhanced immobility. False positives and false negatives can often bescreened by measuring if the compound produces locomotor stimulation orsedation. Strain differences in the tail suspension test have been foundin mice. The tail suspension test has some face validity but itsconstruct validity is rather weak.

Schizophrenia Model

A prepulse inhibition model may be used to assess-the efficacy ofantipsychotic compounds (see Swerdlow and Geyer, Schizophrenia Bulletin24: 285-301, 1998).

Prepulse Inhibition

Prepulse inhibition is the process whereby a relatively mild stimulus,the prepulse, suppresses the response to a strong, startle-elicitingstimulus when the prepulse precedes the startle stimulus by a briefduration (about 10 to 500 milliseconds). Prepulse inhibition is across-species phenomenon (ie, it is present in mammals ranging from miceto humans), yet it is relatively absent among schizophrenic patients.The deficit in PPI in schizophrenic patients is thought to reflect theloss of sensorimotor gating that may lead to sensory flooding andcognitive fragmentation. In this test, mice or rats are administeredcompounds and individually placed into a holder on a transducer platformto measure whole body startle. The holder is housed in a startle chamberwith background white noise. Following a brief habituation period,animals are given multiple trials of a weak auditory prepulse stimululs,followed by a strong auditory startle stimulus. Four types of trials aregiven: prepulse plus startle, prepulse alone, startle alone, and nostimulation. PPI is measured as the amount of inhibition of startlefollowing the prepulse and is expressed as the percentage of basicstartle. As a control, measurements are taken in the no stimulation andprepulse alone trials. PPI is considered a test with good predictive,face and construct validity for schizophrenia. Putative antipsychoticscan be tested alone to determine if they enhance PPI. Alternately,antipsychotics can be screened to determine if they block various agentsthat disrupt PPI (apomorphine, d-amphetamine, PCP, ketamine, DOI).Finally, mutant mice with or without drugs can be screened using the PPIprocedure.

Anxiety Model

An elevated plus maze model may be used to assess the efficacy ofanxiolytic compounds (see Pellow and File, Pharm. Biochem. Behav. 24,525-529, 1986).

Elevated Plus Maze

The elevated plus maze is widely used as an anxiety paradigm thatexamines the conflict between the drive to explore and the aversivenessof heights and open spaces of rats or mice. The maze is a cross made upof two open and two closed arms that is raised above the ground. Thecombination of light, the open arms, and the height is thought toproduce unconditioned fear or anxiety responses in mice or rats. Thetest apparatus is an open top maze constructed of opaque plastic withalternating open and enclosed arms. For rats, each arm is 45-55 cm longand 8-12 cm wide, with the sides of the enclosed arms 35-45 cm high, thejuncture approximately 10×10 cm, and the maze is elevated 45-55 cm abovethe floor. The mouse elevated plus maze consists of two closed arms(15×6×30 cm) and two open arms (1×6×30 cm) forming a cross, with aquadrangular center (6×6cm). The maze is placed 50 cm above the floor.Testing is performed in a room free of noise and distraction. On testdays animals are administered drug or vehicle. If a pretreatment periodis necessary, the animals are returned to the home cage for the durationof the pretreatment time; otherwise, the animals are placed in a clearplastic holding chamber singly or with cage mates for 1-10 minutes priorto test time. Rats are then placed in the center of the maze alwaysoriented in the same direction, either consistently facing an open armor an enclosed arm. For 5-10 minutes, entries into each arm and the timespent in each arm are recorded by the observer(s) or by videotape or acomputer receiving input from a video camera mounted above the maze. Tocount as an entry, all four paws must be inside the arm. If necessary,additional measures of anxiety-related behaviors will be recorded, i.e.,time spent motionless, time spent in the center, time spent grooming,and the number of rears, stretching postures or feces produced.Following testing the animals are returned to the home cages. Whenanimals are placed in the center of the maze, they spend most of theirtime in the closed arms, avoiding the open arms. Anxiolytic drugs, suchas benzodiazepines, will increase the amount of time animals spend inthe open arms. The test is also sensitive to anxiogenic drugs, whichlends strong support for its predictive validity.

Erectile Dysfunction

Drugs affecting erectile function may be tested by measuring the effecton apomorphine-evoked increases in intracavernous pressure in the awakerat as described by Andersson, et al., (J. Urol. 161: 1707-17] 2, 1999).One end of a polyethylene tubing is implanted into the cavernosal spaceof the penis of male Sprague-Dawley rats. After recovery from thesurgery, intracavernous pressure is recorded using a pressure transducerconnected to a multichannel pen-recorder. Erections are induced byadministration of apomorphine (100-250 ug/kg s.c.) with or without testcompound, and the results are compared for the treated group and thenon-treated group.

Female Sexual Dysfunction

Systems to test compounds for the treatment of female sexual dysfunctioninclude in vitro and in situ models using vaginal or clitoral smoothmuscle preparations, histological evaluation, and vaginal blood flowassessments. In vivo studies of sexual responses focus on behavioralparadigms involving lordotic posturing and receptivity, as well asindices of motivation using a dual chamber pacing method (see, e.g.,Hale, et al., Int. J. Impot. Res. 15 Suppl 5: S75-79, 2003).

The present invention is illustrated below with the aid of examples.These illustrations are given solely by way of example and do not limitthe general spirit of the present invention.

EXAMPLES Preparation of 4-(4-Chlorophenyl)-3-methyl-2-oxo-but-3-enoicacid

4-Chlorobenzaldehyde (1.4 g, 10 mmol) was dissolved in MeOH (1 mL) and2-oxobutyric acid (1 g, 9.8 mmol) was subsequently added. A third of a 2M KOH solution (0.84 g) in MeOH (2.5 mL) was added drop wise at a ratethat the temperature of the reaction medium did not rise above 27° C.The remaining alkaline solution was added quickly causing an increase ofthe temperature to 42° C. and the yellow colour of the solution turnsinto orange-red. After approximately five minutes a voluminous andyellow precipitate appeared. After 30 min, water (5 mL) was added andthe organic layer was separated. After extraction with tert-butyl methylether (8 mL), the aqueous phase was acidified with conc. HCl to pH 1 andthoroughly extracted with tert-butyl methyl ether (3×8 mL). The combinedorganic layers were washed with aq. NaCl solution, dried with Na₂SO₄,and evaporated to dryness to afford a cream-white solid (0.88 g, 40%yield). recrystallization of 0.6 g of the crude solid in hexane (40 mL)and ethyl acetate (5 mL) afforded 0.44 g of pure product (80% recovery).

¹H NMR (400 MHz, CDCl₃): δ 2.17 (3H, s, CH₃), 7.44 (4H, d, J 3.28 Hz,ArH), 8.41 (1H, s, CH); ¹³C NMR (100 MHz, CDCl₃): δ 13.2 (CH₃), 129.2(CH), 129.6(C), 131.9 (CH), 133.4 (C), 136.4 (C), 147.6 (CH), 164.4(CO), 187.1 (CO)

Preparation of5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

A mixture of 4-(4-chlorophenyl)-3-methyl-2-oxo-but-3-enoic acid (0.72 g,3.2 mmol) and 2,4-dichlorophenyl hydrazine hydrochloride (0.68 g, 3.2mmol) in glacial acetic acid (10.6 mL) was heated under nitrogenatmosphere to reflux for 4 h. The crude mixture was allowed to cool downto room temperature and poured into ice. The dark mixture was extractedwith dichloromethane, washed with aq. NaCl, dried over Na₂SO₄, andevaporated to dryness to yield 1.18 g of crude product (100% yield) as amixture of two diastereomers. The ratio of the two diastereomers wasdetermined by NMR spectroscopy to be 80:20.

Preparation of5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid methyl ester

Methyl iodide (0.16 mL, 2.25 mmol) was added drop wise to a mixture of5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (0.47 g, 1.27 mmol) and KHCO₃ (0.19 g, 1.9 mmol) in anhydrousdimethylformamide (10 mL) under nitrogen atmosphere. The mixture wasstirred at room temperature under nitrogen overnight (ca 16 h). Waterwas added, the mixture was extracted with ethyl acetate and the combinedorganic layers were thoroughly washed with aq. NaCl solution. Afterdrying over Na₂SO₄ and evaporation under reduced pressure, 0.5 g of thecrude product were obtained. Purification by column chromatography(SiO₂, 40:1 SiO₂, packed with 100% hexane and eluted with a gradient of1% to 5% ethyl acetate) affords 0.045 g (9% yield) of the minor isomer(RS and SR as a racemic mixture, trans isomer) and 0.23 g (48% yield) ofthe major isomer (RR and SS as a racemic mixture, cis isomer).

Example 24 Minor Isomer:trans-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid methyl ester

¹H NMR (400 MHz, CDCl₃): δ 1.49 (3H, d, J 7.6 Hz, CH₃), 3.51 (1H, m,CH), 3.90 (3H, s, OCH₃), 5.32 (1H, d, J 5.6 Hz, CH), 7.03-7.10 (3H, m,ArH), 7.20 (2H, ap d J 8.4 Hz, ArH), 7.25-7.28 (2H, m, ArH)

¹³C NMR (100 MHz, CDCl₃): δ 18.4 (CH₃), 49.6 (CH), 52.5 (OCH₃), 75.5(CH), 126.2 (CH), 126.7 (C), 127.8 (CH), 128.1 (CH), 129.3 (CH), 130.4(CH), 134.5 (C), 137.6 (C), 139.1 (C), 145.2 (C), 162.8 (CO)

MS (M+H)⁺: 398

Example 23 Major Isomer:cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid methyl ester

¹H NMR (400 MHz, CDCl₃): δ 0.94 (3H, d, J 7.2 Hz, CH₃), 3.80 (1H, m,CH), 3.88 (3H, s, OCH₃), 5.82 (1H, d, J 11.2 Hz, CH), 7.04-7.10 (3H, m,ArH), 7.22 (2H, m, ArH), 7.24-7.29 (2H, m, ArH)

¹³C NMR (100 MHz, CDCl₃): δ 17.8 (CH₃), 49.5 (CH), 52.7 (OCH₃), 75.7(CH), 126.2 (CH), 127.7 (C), 127.9 (CH), 129.4 (CH), 130.4 (CH), 130.8(C), 134.4 (C), 137.9 (C), 139.0 (C), 144.8 (C), 162.8 (CO)

MS (M+H)⁺: 398

Hydrolysis of the Racemic Mixture of (RR)- and(SS)-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid methyl ester

Aq. 2 M NaOH (6.4 mL) was added to a solution of the racemic mixture of(RR)- and(SS)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid methyl ester (0.36 g, 0.9 mmol) in THF (6.4 mL). The mixture wasleft to stir at room temperature for 3 h (until TLC showed disappearanceof the starting material). Water was added and the reaction mixture wasconcentrated under reduced pressure. The residue was washed once withEt₂O and the aqueous phase acidified to pH 1 with 1 M HCl. Extractionwith ethyl acetate, drying with Na₂SO₄ and concentration to drynessyielded pure acid (0.23 g, 68% yield).

Example 19 Major Isomer:cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

¹H NMR (400 MHz, CHLOROFORM-d) δ ppm 0.96 (d, J=7.42 Hz, 3H) 3.82 (td,J=11.72, 7.42 Hz, 1H) 5.91 (d, J=11.72 Hz, 1H) 7.04 (d, J=8.60 Hz, 2H)7.11 (dd, J=8.60, 2.34 Hz, 1H) 7.21-7.30 (m, 4H)

¹³C NMR (100 MHz, CDCl₃): δ 13.6 (CH₃), 43.5 (CH), 72.0 (CH), 124.9(CH), 127.6 (CH), 129.1 (CH), 129.6 (CH), 130.9 (CH), 131.3 (C), 132.7(C), 134.5 (C), 138.7 (C), 144.6 (C), 165.9 (CO).

MS (M+H)⁺: 384

Hydrolysis of the Racemic Mixture of (RS)- and(SR)-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid methyl ester

The hydrolysis was carried out as described above for the racemicmixture of (RR)- and(SS)-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid methyl ester

Example 20 Minor Isomer:trans-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

¹H NMR (400 MHz, CHLOROFORM-d) δ ppm 1.52 (d, J=7.03 Hz, 3H) 3.52 (m,1H) 5.39 (d, J=5.47 Hz, 1H) 7.08 (ddd, J=13.92, 5.62, 5.28 Hz, 3H)7.14-7.34 (m, 4H)

¹³C NMR (100 MHz, CDCl₃): δ 18.4 (CH₃), 48.9 (CH), 76.2 (CH), 126.4(CH), 126.7 (C), 127.8 (CH), 128.0 (CH), 129.5 (CH), 130.5 (CH), 131.5(C), 134.7 (C), 137.6 (C), 138.6 (C), 144.2 (C), 166.5 (CO).

MS (M+H)⁺: 384

Preparation of 4-(4-Chlorophenyl)-3-methyl-2-oxo-but-3-enoic acid methylester

4-(4-Chlorophenyl)-3-methyl-2-oxo-but-3-enoic acid (0.13 g, 0.58 mmol)was dissolved in Et₂O (0.8 mL) and EtOH (1.2 mL) and the solution wascooled down to 0° C. TMSCH₂N₂ (0.43 mL of a 2 M solution in Et₂O, 0.87mmol) was added drop wise and the mixture was stirred at 0° C. for 1 h.A second portion of TMSCH₂N₂ (0.2 mL of a 2 M solution in Et₂O, 0.40mmol) was added and the reaction was allowed to reach room temperature.After 30 min, the solvents were evaporated to dryness and the residuewas taken up in a mixture of Et₂O/hexane 1:1 (10 mL). The organic layerwas washed with 2% aq. HCl (10 mL), aq. NaHCO₃ (10 mL) and aq. NaCl (10mL), dried over Na₂SO₄ and concentrated to dryness to give pure product(68 mg, 49% yield).

Preparation of5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid methyl ester

A mixture of 4-(4-chlorophenyl)-3-methyl-2-oxo-but-3-enoic acid methylester (0.4 g, 1.68 mmol) and 2,4-dichlorohydrazine hydrochloride (0.356g, 1.68 mmol) in glacial acetic acid (4 mL) was heated at reflux undernitrogen atmosphere for 4 h. The reaction mixture was then allowed tocool down to room temperature and poured into ice. The dark mixture wasextracted with dichloromethane, washed with aq. NaCl, dried over Na₂SO₄and evaporated to dryness to yield the crude product (0.64 g, 95% yield,as a mixture of two diastereomers). Purification by columnchromatography (SiO₂, 40:1 SiO₂, packed with 100% hexane and eluted witha gradient of 1% to 5% ethyl acetate) of 0.5 g of crude product afforded0.051 g of the minor isomer (RS and SR as a racemic mixture) and 0.20 gof the major isomer (RR and SS as racemic mixture).

Preparation of Example 1cis-5-(4-Chloro-phenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide Hydrochloride

5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (0.160 g, 0.417 mmol) was dissolved in toluene (4 mL) and waspartially distilled at atmospheric pressure to eliminate water traces.The resulting solution was cooled to 75-85° C. DMF was added (2 drops)as a catalyst and thionyl chloride (0.060 mL, 0.5 mmol) was added dropby drop. The solution was stirred until formation of the acid chloridewas complete (monitoring by IR). The mixture was cooled to 20-25° C. andwas added drop wise to a solution of 1-aminopiperidine (0.053 mL, 0.500mmol), dichloromethane (5 mL) and N,N-diisopropylethylamine (0.170 mL, 1mmol) under nitrogen at a temperature between 5-10° C. After completeaddition the mixture was warmed to 20-25° C. and stirred overnight. Theorganic layer was washed with water (3×5 mL), a sat. NaHCO₃ solution(3×25 mL) and again with water (3×mL). The combined organic layers weredried with Na₂SO₄, filtered and concentrated under vacuum to give asolid (130 mg, 68% yield).

The crude solid was dissolved in ethyl acetate and a 2.8 M HCl solutionin ethanol was added drop wise to form the hydrochloride which wasobtained as a beige solid (82 mg, 49% yield).

¹H NMR (400 MHz, METHANOL-d₄) δ ppm 0.94 (d, J=7.42 Hz, 3H) 1.68 (br,2H) 1.98 (dt, J=11.28, 5.59 Hz, 4H) 3.53 (br, 4H) 3.90 (td, J=11.53,7.42 Hz, 1H) 5.99 (d, J=11.53 Hz, 1H) 7.16 (d, J=8.40 Hz, 2H) 7.20-7.29(m, 3H) 7.36-7.48 (m, 2H)

MS (M+H)⁺: 466

Example 2trans-5-(4-Chloro-phenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide Hydrochloride

5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (0.190 g, 0.50 mmol) was dissolved in toluene (4 mL) and waspartially distilled at atmospheric pressure to eliminate water traces.The resulting solution was cooled to 75-85° C. DMF was added (2 drops)as a catalyst and thionyl chloride (0.060 mL, 0.5 mmol) was added dropby drop. The solution was stirred until formation of the acid chloridewas complete (monitoring by IR). The mixture was cooled to 20-25° C. andwas added drop wise to a solution of 1-aminopiperidine (0.0623 mL, 0.57mmol), dichlorornethane (5 mL) and N,N-diisopropylethylamine (0.197 mL,1.15 mmol) under nitrogen at a temperature between 5-10° C. Aftercomplete addition the mixture was warmed to 20-25° C. and stirredovernight. The organic layer was washed with water (3×5 mL), a sat.NaHCO₃ solution (3×25 mL) and again with water (3×5 mL). The combinedorganic layers were dried with Na₂SO₄, filtered and concentrated undervacuum to give a solid. The crude solid was dissolved in ethyl acetateand a 2.8 M HCl solution in ethanol was added drop wise to form thehydrochloride which was obtained as a beige solid (120 mg, 50% yield).

¹H NMR (400 MHz, DMSO-d₆) δ ppm 1.38 (d, J=7.03 Hz, 3H) 1.42 (m, 2H)1.71 (m, 4H) 3.12 (m, 4H) 3.42 (dt, J=13.38, 5.86 Hz, 1H) 5.36 (d,J=5.86 Hz, 1H) 7.19 (d, J=8.21 Hz, 2H) 7.31 (d, J=8.60 Hz, 3H) 7.49 (d,J=2.34 Hz, 1H) 7.53 (d, J=8.60 Hz, 1H) 10.49 (s, 1H)

MS (M+H)⁺: 466

The following compounds were prepared according to the processesdescribed above. Those skilled in the art are familiar with the startingmaterials that are needed to obtain said compounds.

Preparation of Compounds of General Formula II

Acid of general formula VI (1.1 equivalents) was added in portions to asolution of 0.5 M aqueous NaOH (1.5 equivalents) under N₂ at roomtemperature. The reaction was then left stirring for 5 min and asolution of a compound of general formula VII (1 equivalent) in abs.EtOH (0.9 M) was then slowly added (10 mL/h). The reaction was leftstirring at 25° C. overnight.

Water was added and the solvent was evaporated under reduced pressure toeliminate the excess of EtOH. The solution was then washed with tolueneand the solvent was again evaporated. The aqueous solution was thencooled in an ice bath and conc. aqueous HCl (0.2 mL of conc. HCl per mLof base) were slowly added while stirring. A white solid precipitatedfrom the solution which was kept at 0° C. for another hour. The solidwas filtered under vacuum through a sintered funnel (porosity 3) anddried at 40° C. under vacuum.

As a example, if the starting material was 2-oxobutyric acid, the yieldrange for this reaction condensation was around 60-86%. However, if thestarting material was 2-oxopentanoic acid (oxovaleric acid) instead of2-oxobutyric acid, the yield of the reaction was slightly lower (around40-60%)

Compound A1 (E)-4-(4-chlorophenyl)-3-methyl-2-oxobut-3-enoic acid

¹H NMR (400 MHz, CDCl₃): δ 2.17 (3H, s, CH₃), 7.44 (4H, ap d, J=3.28 Hz,ArH), 8.41 (1H, s, CH).

Compound A2 (E)-4-(4-bromophenyl)-3-methyl-2-oxobut-3-enoic acid

¹H NMR (400 MHz, CD₃OD): δ 1.99 (3H, s, CH₃), 7.36 (2H, d, J=8.5 Hz,ArH), 7.40 (1H, s, CH), 7.53 (2H, d, J=8.5 Hz, ArH).

Compound A3 (E)-4-(4-fluorophenyl)-3-methyl-2-oxobut-3-enoic acid

¹H NMR (300 MHz, DMSO-d₆): δ 2.18 (3H, s, CH₃), 7.20 (2H, m), 7.53 (2H,m), 8.26 (1H, s, CH).

Compound A4 (E)-4-(4-methoxyphenyl)-3-methyl-2-oxobut-3-enoic acid.

This compound was prepared following the method described above butusing instead 3 eq. of NaOH.

¹H NMR (200 MHz, CDCl₃): δ 2.09 (3H, s, CH₃), 3.84 (3H, s, OCH₃), 7.01(2H, d, J=8.8 Hz, ArH), 7.50 (1H, s, CH), 7.52 (2H, d, J=8.8 Hz, ArH).

Compound A5 (E)-3-methyl-2-oxo-4-phenylbut-3-enoic acid

¹H NMR (200 MHz, CDCl₃): δ 2.19 (3H, s, CH₃), 7.33-7.51 (5H, m, ArH),8.36 (1H, s, CH)

Compound A6 (E)-4-(4-bromophenyl)-3-ethyl-2-oxobut-3-enoic acid

¹H NMR (400 MHz, CDCl₃): δ 1.16 (3H, t, J 7.5 Hz, CH₃), 2.62 (2H, q, J7.5 Hz, CH₂), 7.35 (2H, d, J 8.4 Hz, ArH), 7.59 (2H, d, J 8.4 Hz, ArH),8.23 (1H, s, CH).

Compound A7 (E)-4-(4-chlorophenyl)-3-ethyl-2-oxobut-3-enoic acid

¹H NMR (400 MHz, CDCl₃): δ 1.16 (3H, t, J 7.2 Hz, CH₃), 2.61 (2H, q, J15.6 Hz, J 7.2 Hz ArH), 7.44 (4H, m, ArH), 7.85 (1H, bs, CH).

Compound A8 (E)-4-(5-chlorothiophen-2-yl)-3-methyl-2-oxobut-3-enoic acid

¹H NMR (400 MHz, CDCl₃): δ 2.09 (3H, s, CH₃), 7.10 (1H, d, J 4.8, ArH),7.32 (1H, d, J 4.8 Hz, ArH), 7.64 (1H, s, ArH).

Compound A9 (E)-4-(5-bromothiophen-2-yl)-3-methyl-2-oxobut-3-enoic acid

¹H NMR (400 MHz, CDCl₃): δ 2.19 (3H, d, J 0.9 Hz, CH₃), 7.19 (1H, d, J3.7 Hz thiophene H), 7.27 (1H, d, J 3.7 Hz, thiophene H), 8.74 (1H, bs,CH).

Compound A10 (E)-3-methyl-2-oxo-4-(thiophen-2-yl)but-3-enoic acid

¹H NMR (400 MHz, CDCl₃): δ 2.25 (3H, s, CH₃), 7.22 (1H, dd, J 5.1, 3.6Hz, ArH), 7.52 (1H, d, J 3.6 Hz, ArH), 7.72 (1H, d, J 5.1, Hz, ArH),8.68 (1H, s, CH).

Preparation of Compounds of General Formula V

A suspension of a compound of general formula III (1 equivalent) inglacial acetic acid (40 equivalents) was heated at 80° C. under nitrogenatmosphere. When the suspension became a solution, a solution of acid ofgeneral formula II (1 equivalent) in acetic acid (20 equivalents) wasadded and the solution was left stirring at 80° C. for 2 h. The reactionmixture was allowed to crystallise at 0-4° C. overnight after partialevaporation of acetic acid. The beige solid formed was filtered offunder vacuum through a sintered funnel (porosity 4) and washed severaltimes with water. This crystallization process led to the majordiastereomeric acid with cis configuration. The yield range for thecyclization with hydrazine to obtain the main diastereomer was around46-80%.

The reaction mixture can also be cooled down to room temperature andpoured through an addition funnel into water which is cooled in an icebath with magnetically stirring. The addition must be slow and at leastdouble volume of water per volume of acetic acid is required. Aprecipitate should form, but in the case a gum starts to form, it shouldbe filtered and the rest of the material should be poured into anotherlarge volume of water. The solid obtained is suspended in water severaltimes and filtered off until the pH of the water was above 3. This solidalso corresponds to the cis form.

Alternatively, the dark mixture can be extracted with dichloromethanewashed thoroughly with H₂O, dried over Na₂SO₄ and evaporated to dryness.Recrystallisation of the crude material from toluene (3 to 4 mL oftoluene per gram of material) allows the recovery of the majordiastereomer with cis configuration.

Formation of the methyl esters as described in the method above,followed by purification by column chromatography, allows for theseparation of the two diastereoisomers.

Preparation of Compounds of General Formula IV with Trans-configuration

A solution of NaNO₂ (0.460 mg, 6.68 mmol) in water (0.8 ml) was added toa stirred solution of a an amine, wherein R² denotes an unsubstituted orat least mono-substituted phenyl radical, (6.17 mmol) and concentratedhydrochloric acid (1.5 ml) in ice (1.5 ml). The reaction mixture wasstirred for 1 h at 0-5° C. and added to a cold mixture of NaOAc (1.64 g,19.6 mmol), ethanol (26 ml) and ethyl-2-chloro-3-oxobutanoate (1.0 g,6.06 mmol). The reaction mixture was left stirring for 1 hour until aprecipitate formed which was collected by filtration, washed withethanol and dichloromethane and dried in vacuo to give the yellow solidethyl of general formula XXIII (70-80% yield), which was used in thenext step without any further purification.

Triethylamine (2.8 eq) was added to a solution of a compound of generalformula XXIII (1 eq) and a disubstituted (E)-alkene of general formulaXXII (3 eq) in toluene, and the reaction mixture was stirred at refluxtemperature for 1 hour. A precipitate formed which was removed byfiltration after cooling to room temperature. The filtrate wasconcentrated and purified using a Combiflash system from Isco, elutedwith cyclohexane and ethyl acetate (in a gradient program until 30%AcOEt), to obtain ethyl ester derivatives of compounds of generalformula IV, (˜40% yield).

Ethyl esters derivatives of compounds of general formula IV werehydrolysed in the presence of aqueous 2 M NaOH (2 eq) andtetrahydrofuran for 4 hours. Tetrahydofuran was partially removed byevaporation, 1 M aqueous HCl was added until pH was below 3 and theaqueous mixture was extracted with ethyl acetate, dried over Na₂SO₄,filtered and concentrated in vacuo to yield a white solid identified ascarboxylic acid of general formula IV (85% yield).

The enantiomers of each acid (cis or trans) can be separated by chiralHPLC or by crystallization of the diastereomeric salts formed withchiral amines.

Example 199cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

IR (NaCl film, cm⁻¹):2976, 1683, 1541, 1486, 1385, 1270, 1242, 1116.

¹H NMR (400 MHz, CDCl₃): δ 0.96 (3H, d, J=7.3 Hz, CH₃), 3.82 (1H, qd,J=11.9, 7.3, 7.3, 7.3 Hz, 1H), 5.88 (1H, d, J=11.9 Hz, CH), 6.99 (2H, apd, J=8.4 Hz, ArH), 7.12 (1H, dd, J=8.7, 2.3 Hz, 1H), 7.17 (1H, m, ArH),7.27 (1H, m, ArH), 7.39 (2H, d, J=8.4 Hz, ArH).

Example 221cis-5-(4-fluorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

IR (NaCl film, cm⁻¹): 2978, 1682, 1486, 1471, 1264, 1117.

¹H NMR (400 MHz, CHLOROFORM-d) δ ppm 0.97 (d, J=7.42 Hz, 3H) 3.82 (td,J=11.72, 7.42 Hz, 1H) 5.91 (d, J=12.0 Hz, 1H), 6.95 (m, 2H), 7.10 (m,3H), 7.20 (d, J=9.0 Hz, 1H), 7.30 (d, J=3.0 Hz, 1H).

Example 261cis-5-(4-methoxyphenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

IR (NaCl film, cm⁻¹): 2936, 2836, 1681, 1612, 1512, 1480, 1460, 1248,1113.

¹H NMR (400 MHz, CDCl₃): δ 0.97 (3H, d, J=7.3 Hz, CH₃), 3.74 (3H, s,OCH₃), 3.80 (1H, m, 1H), 5.88 (1H, d, J=11.8 Hz, CH), 6.76 (2H, ap d,J=8.6 Hz, ArH), 7.00 (2H, d, J=8.6, ArH), 7.09 (1H, dd, J=8.6, 2.3 Hz,ArH), 7.16-7.28 (2H, m, ArH).

Example 185cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

IR (NaCl film, cm⁻¹): 2969, 1682, 1480, 1452, 1270, 1236, 1151, 1106.

¹H NMR (400 MHz, CDCl₃): δ 0.69 (3H, t, J 7.4 Hz, CH₃), 1.28-1.34 (1H,m, CHH), 1.95-2.00 (1H, m, CHH), 3.68 (1H, ddd, J=11.5, 9.7, 4.0 Hz,CH), 5.92 (1H, d, J 11.5Hz, CH), 7.02(2H, ap d, J 8.4 Hz, ArH), 7.09(1H, dd, J=8.7, 2.4 Hz, ArH), 7.20 (1H, d, J 8.7 Hz, ArH), 7.28 (1H, d,J 2.4 Hz, ArH), 7.36 (2H, ap d, J 8.4 Hz, ArH);

¹³C NMR (100 MHz, CDCl₃): δ 12.4 (CH₃), 20.0 (CH₂), 50.5 (CH₃), 52.3(OCH₃), 72.0 (CH), 122.5 ©, 124.8 (CH), 127.4 ©, 127.5 (CH), 129.9 (CH),130.4 (CH), 131.1 ©, 131.7 (CH), 132.7 ©, 138.5 ©(, 143.8 ©, 165.4 (CO).

Example 21cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

¹H NMR (400 MHz, CDCl₃): δ 0.70 (3H, t, J 7.2 Hz, CH₃), 1.31 (1H, m,CHH), 2.01 (1H, m, CHH, 3.68 (1H, m, CH), 5.92 (1H, d, J 11.6 Hz, CH),7.07-7.31 (7H, m, ArH).

Example 22trans-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

¹H NMR (400 MHz, CDCl₃): δ 1.08 (3H, t, J 7.2 Hz, CH₃), 1.90 (1H, m,CHH), 1.96 (1H, m, CHH, 3.50 (1H, m, CH), 5.59 (1H, d, J 4.80 Hz, CH),7.01-7.31 (7H, m, ArH).

Example 200trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

¹H NMR (400 MHz, CDCl₁₃): δ 1.52 (3H, d, J=7.1 Hz, CH₃), 3.52 (1H, m,1H), 5.35(1H, d, J=5.8 Hz, CH), 7.00 (2H, ap d, J=8.4 Hz, ArH), 7.10(1H, dd, J=8.7, 2.3 Hz, 1H), 7.22 (1H, d, J=8.7, ArH), 7.27 (1H, d,J=2.3 Hz, ArH), 7.37 (2H, d, J=8.4 Hz, ArH).

Example 373cis-1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

¹H NMR (400 MHz, CDCl₃): δ 0.96 (3H, d, 7.6 Hz, CH₃), 3.82 (1H, m, CH),3.88 (3H, s, OCH₃), 5.91 (1H, d, J 11.6 Hz, CH), 7.09-7.31 (8H, m, ArH)

Example 374trans-1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

IR (NaCI film, cm⁻¹): 3400-2800, 1680, 1479, 1456, 1108

¹H NMR (400 MHz, CDCl₃): δ 1.53 (3H, d, 7.2 Hz, CH₃), 3.57 (1H, m, CH),3.90 (3H, s, OCH₃), 5.37 (1H, d, J 5.6 Hz, CH), 7.06-7.28 (8H, m , ArH)

Example 361cis-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

IR (NaCI film, cm⁻¹): 3400-2800, 1684, 1479, 1447, 1107.

¹H NMR (400 MHz, CDCl₃): δ 1.24 (3H, d, J 7.2, CH₃), 3.81 (1H, m, CH),6.09 (1H, d, J 12.0, CH), 6.64 (2H, ap dd, J₁ 12.0, J₂ 3.8 Hz, ArH),7.16 (1H, dd, , J₁ 8.8, J₂ 2.2 Hz, ArH), 7.32 (1H, d J 2.2 Hz, ArH),7.34 (1H, aps, ArH), 7.36 (1H, aps, ArH).

Example 362trans-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

IR (NaCi film, cm⁻¹): 3400-2800, 1682, 1569, 1544, 1479, 1448, 1246,1105.

¹H NMR (400 MHz, CDCl₃): δ 1.50 (3H, d, J 7.1 Hz, CH₃), 3.64 (1H, m,CH), 5.6 (1H, d, J 3.9 Hz, CH), 6.60 (2H, aps, ArH), 7.12 (1H, dd, J₁8.8, J₂ 2.3 Hz, ArH), 7.27 (1H, m, ArH), 7.33 (1H, d, J 2.3 Hz, ArH).

Example 88cis-5-(5-bromothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid

IR (NaCI film, cm⁻¹): 3400-2800, 1682, 1569, 1545, 1479, 1459, 1245,1105.

¹H NMR (400 MHz, CDCl₃): δ 1.23 (3H, d, J 7.2 Hz, CH₃), 3.81 (1H, m,CH), 6.11 (1H, d, J 11.6 Hz, CH), 6.61 (1H, d, J 3.9 Hz, ArH), 6.80 (1H,d, J 4.4 Hz, ArH), 7.16 (1H, dd, J₁ 8.4 Hz, J₂ 3.0 Hz, ArH), 7.30-7.34(2H, m, ArH).

¹³C NMR (100 MHz, CDCl₃): δ 12.3 (CH₃), 43.7 (CH), 69.5 (CH), 112.9 ©,125.9 (CH), 126.8 ©, 127.8 (CH), 128.7 (CH), 129.7 (CH), 130.5 (CH),131.8 ©, 137.8 ©, 138.6 ©, 144.9 ©, 164.5 (CO).

Example 367cis-1-(2,4-dichlorophenyl)-4-methyl-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-carboxylicacid

IR (NaCI film, cm⁻¹): 3400-2800, 1682, 1567, 1543, 1479, 1449, 1245,1108.

¹H NMR (400 MHz, CDCl₃): δ 1.19 (3H, d, J 7.2 Hz, CH₃), 3.83 (1H, m,CH), 6.22 (1H, d, J 11.2 Hz, CH), 6.84 (2H, m, ArH), 7.12 (2H, m, ArH),7.29 (1H, d, J 2.3, ArH), 7.34 (1H, d, J 8.8 Hz, ArH).

Preparation of Compounds of General Formula V

A compound of general formula IV (15 mmol) was dissolved in 120 mL ofdry toluene and thionyl chloride (18 mmol) was added. The mixture washeated to 80° C. for 2.5 hours. The solvent was removed under reducedpressure and the resulting crude residue was used without any furtherpurification.

Cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbonylchloride

IR (NaCl film, cm⁻¹): 1732, 1700, 1533, 1478, 1212, 826.

Cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbonylchloride

IR (NaCl film, cm⁻¹): 1731, 1527, 1477, 1204, 1153, 1132, 825, 802.

Cis-5-(4-fluorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbonyl chloride

IR (NaCl film, cm⁻¹): 1731, 1509, 1478, 1227, 1153, 1132, 853, 803.

Cis-5-(4-methoxyphenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3carbonylchloride

IR (NaCl film, cm⁻¹): 1730, 1611, 1512, 1477, 1271, 1250, 1034, 831,800.

Cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carbonyl chloride

IR (NaCl film, cm⁻¹): 1728, 1526, 1478, 1227, 1200,1153, 1129, 834, 801.

Cis-5-(5-chlorothiophen-2-yl)1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbonyl chloride

IR (NaCl film, cm⁻¹): 1732, 1528, 1477, 1446, 1226, 1112, 808.

Trans-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbonylchloride

IR (NaCl film, cm⁻¹): 1730, 1531, 1479, 1204, 1122, 806.

Cis-5-(5-bromothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbonylchloride

IR (NaCl film, cm⁻¹): 1732, 1528, 1477, 1109, 806

cis-1-(2,4dichlorophenyl)-4-methyl-5-(thiophen-2-yl)4,5-dihydro-1H-pyrazole-3-carbonylchloride

IR (NaCl film, cm⁻¹): 1731, 1527, 1477, 1224, 1111, 803.

Preparation of Compounds of General Formula I

A compound of general formula R³—H (5.6 mmol) and triethylamine (4 mL)were dissolved in dichloromethane (25 mL) under nitrogen atmosphere. Theresulting mixture was cooled to 0° C. and a solution of a compound ofgeneral formula V (4.6 mmol) in dichloromethane (15 mL) was addeddropwise. The resulting reaction mixture was stirred at room temperature(approximately 25° C.) overnight, washed with water, saturated aqueoussolution of sodium bicarbonate and again with water, dried over sodiumsulfate, filtered and evaporated to dryness in a rotavapor. The residuewas crystallized from ethanol, ethyl acetate or acetone. Thecrystallized solid was removed via filtration and the mother liquorswere concentrated to yield a second fraction of crystallized product.The two fractions were combined to give the desired product (yieldrange: 60-80%). Alternatively, a solution of 2 N HCl in diethyl ether or2.8 N in ethanol was added to form the respective hydrochloride, whichwas collected by filtration.

Example 1cis-5-(4-Chlorophenyl)-1-(2,4dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide hydrochloride

¹H NMR (400 MHz, METHANOL-d₄) δ ppm 0.94 (d, J=7.42 Hz, 3H) 1.68 (br,2H) 1.98 (dt, J=11.28, 5.59 Hz, 4H) 3.53 (br, 4H) 3.90 (td, J=11.53,7.42 Hz, 1H) 5.99 (d, J=11.53 Hz, 1H) 7.16 (d, J=8.40 Hz, 2H) 7.20-7.29(m, 3H) 7.36-7.48 (m, 2H)

MS (M+H)⁺: 466

Example 2trans-5-(4-Chloro-phenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide hydrochloride

¹H NMR (400 MHz, DMSO-d₆) δ ppm 1.38 (d, J=7.03 Hz, 3H) 1.42 (m, 2H)1.71 (m, 4H) 3.12 (m, 4H) 3.42 (dt, J=13.38, 5.86 Hz, 1H) 5.36 (d,J=5.86 Hz, 1H) 7.19 J=8.21 Hz, 2H) 7.31 (d, J=8.60 Hz, 3H) 7.49 (d,J=2.34 Hz, 1H) 7.53 (d, J=8.60 Hz, 1H) 10.49(s, 1H)

MS (M+H)⁺: 466

Example 15cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide

¹H NMR (300 MHz, CHLOROFORM-d): δ ppm 0.97 (d, J=7.18 Hz, 3H) 3.08 (t,J=7.98 Hz, 2H) 3.67 (t, J=7.98 Hz, 2H) 3.86 (dd, J=11.06, 7.40 Hz, 1H)5.69 (d, J=11.28 Hz, 1H) 6.73 (d, J=7.76 Hz, 1H) 6.88 (t, J=7.40 Hz, 1H)7.02 -7.12 (m, 5H) 7.15 (d, J=7.76 Hz, 2H) 7.24 (s, 1H) 7.33 (d, J=1.61Hz, 1H) 7.99 (s, 1H)

MS (M+H(⁺: 499

Example 113cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(2-methylindolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide

¹H NMR (300 MHz, DMSO-d₆): δ ppm 0.81 (t, J=7.40 Hz, 3H) 1.29 (d, J=5.86Hz, 3H) 2.54-2.65 (m, 1H) 3.14 (m, 1H) 3.92 (m, 2H) 5.99 (d, J=11.28 Hz,1H) 6.45 (dd, J=7.54, 2.86 Hz, 1H) 6.68-6.82 (m, 1H) 6.96-7.23 (m, 4H)7.30-7.36 (m, 3H) 7.48 (d, J=2.05 Hz, 1H) 7.71 (d, J=8.79 Hz, 1H) 10.09(s, 1H)

MS (M+H)⁺: 513

Example 215cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazol-3-carboxamide

¹H NMR (300 MHz, DMSO-d₆): δ ppm 0.80 (d, J=7.18 Hz, 3H) 2.96 (t, J=8.50Hz, 2H) 3.59 (t, J=8.50 Hz, 2H) 3.89 (dd, J=11.13, 7.18 Hz, 1H) 5.95 (d,J=11.13 Hz, 1H) 6.49 (d, J=7.62 Hz, 1H) 6.75 (t, J=7.03 Hz, 1H)6.99-7.14 (m, 4H) 7.31 (dd, J=8.79, 2.49 Hz, 1H) 7.42-7.50 (m, 3H) 7.66(d, J=8.79 Hz, 1H) 10.19 (s, 1H)

MS (M+H)⁺: 543

Example 235cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide

¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.80 (d, J7.32 Hz, 3H) 2.96 (t, J=8.50Hz, 2H) 3.59 (t, J=8.50 Hz, 2H) 3.87 (dd, J=11.13, 7.32 Hz, 1H) 5.96 (d,J=1 1.13 Hz, 1H) 6.49 (d, J=7.62 Hz, 1H) 6.75 (t, J=7.40 Hz, 1H)7.00-7.19 (m, 6H) 7.30 (dd, J=8.72, 2.42 Hz, 1H) 7.47 (d, J=2.34 Hz, 1H)7.67 (d, J=8.79 Hz, 1H) 10.18 (s, 1H)

MS (M+H)⁺: 483

Example 279cis-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide

¹H NMR (300 MHz, CHLOROFORM-d) δ ppm 0.99 (d, J=7.18 Hz, 3H) 3.08 (t,J=7.98 Hz, 2H) 3.68 (t, J=7.91 Hz, 2H) 3.76 (s, 3H) 3.83 (dd, J=11.13,7.18 Hz, 1H) 5.68 (d, J=11.13 Hz, 1H) 6.79 (d, J=8.50 Hz, 2H) 6.74 (d,J=7.76 Hz, 1H) 6.88 (t, J=7.40 Hz, 1H) 7.02-7.09 (m, 4H) 7.16 (d, J=7.47Hz, 2H) 7.32 (s, 1H) 8.01 (s, 1H)

MS (M+H)⁺: 495

Example 123cis-5-(4-chlorophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3carboxamide

¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.76 (d, J=7.18 Hz, 3H) 1.39-1.70 (m,10H) 1.78 (m, 2H) 3.83 (m, 2H) 5.89 (d, J=10.99 Hz, 1H) 7.14 (d, J=8.35Hz, 2H) 7.32 (m, 3H) 7.49 (d, J=2.34 Hz, 1H) 7.62 (d, J=8.79 Hz, 1H)8.04 (d, J=8.06 Hz, 1H)

MS (M+H)⁺: 478

Example 193cis-5-(4-bromophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4methyl-4,5-dihydro-1H-pyrazole-3-carboxamide

¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.74 (d, J=7.18 Hz, 3H) 1.35-1.66 (m,10H) 1.78 (m, 2H) 3.72-3.90 (m, 2H) 5.85 (d, J=10.99 Hz, 1H) 7.06 (d,J=8.35 Hz, 2H) 7.30 (dd, J=8.72, 2.27 Hz, 1H) 7.44 (d, J=8.35 Hz, 2H)7.47 (d, J=2.20 Hz, 1H) 7.60 (d, J=8.79 Hz, 1H) 8.02 (d, J=8.20 Hz, 1H)

MS (M+H)⁺: 522

Example 231 cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide

¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.75 (d, J=7.32 Hz, 3H) 1.36-1.67 (m,10H) 1.71-1.85 (m, 2H) 3.70-3.90 (m, 2H) 5.86 (d, J=10.99 Hz, 1H)7.02-7.18 (m, 4H) 7.29 (dd, J=8.79, 2.34 Hz, 1H) 7.46 (d, J=2.34 Hz, 1H)7.61 (d, J=8.79 Hz, 1H) 8.02 (d, J=8.20 Hz, 1H)

MS (M+H)⁺: 462

Example 275cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide

¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.75 (d, J =7.32 Hz, 3H) 1.36-1.67 (m,10H) 1.75-1.86 (m, 2H) 3.65 (s, 3H) 3.72.(dd, J=10.99, 7.32 Hz, 1H) 3.82(dd, J=8.72, 4.47 Hz, 1H) 5.79 (d, J=10.99 Hz, 1H) 6.77 (d, J=8.64 Hz,2H) 7.01 (d, J=8.64 Hz, 2H) 7.27 (dd, J=8.79, 2.34 Hz, 1H) 7.44 (d,J=2.34 Hz, 1H) 7.61 (d, J=8.79 Hz, 1H) 7.99 (d, J=8.20 Hz, 1H)

MS (M+H)⁺: 474

Example 128(+)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide

¹H NMR (300 MHz, CHLOROFORM-d) δ ppm 0.94 (d, J=7.32 Hz, 3H) 1.19-1.45(m, 4H) 1.76 (m, 2H) 2.00 (m, 1H) 2.09 (m, 1H) 3.43 (m, 1H) 3.78 (m, 2H)5.66 (d, J=11.28 Hz, 1H) 6.65 (d, J=7.32 Hz, 1H) 7.00-7.15 (m, 4H) 7.24(m, 2H) 7.33 (s, 1H)

MS (M+H)⁺: 480

Example 129(−)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide

¹H NMR (300 MHz, CHLOROFORM-d) δ ppm 0.93 (d, J=7.32 Hz, 3H) 1.24-1.40(m, 4H) 1.75 (m, 2H) 2.06 (m, 2H) 3.39 (m, 1H) 3.75 (m, 2H) 5.64 (d,J=11.13 Hz, 1H) 6.68 (d, J=7.32 Hz, 1H) 7.00-7.13 (m, 4H) 7.23 (d,J=8.50 Hz, 2H) 7.35 (d, J=2.20 Hz, 1H)

MS (M+H)⁺: 480

Example 108 cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta-[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride

¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.79 (d, J=7.18 Hz, 3H) 1.49 (d, J=7.76Hz, 2H) 1.61 (m, 4H) 2.66 (br. S., 2H) 2.86 (m, 2H) 3.54 (br. S., 2H)3.85 (m, 1H) 5.96 (d, J=11.28 Hz, 1H) 7.17 (d, J=8.35 Hz, 2H) 7.35 (m,3H) 7.55 (d, J=2.20 Hz, 1H) 7.62 (d, J=8.64 Hz, 1H) 10.52 (br. S., 1H)

MS (M+H)⁺: 491

Example 213 cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta-[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride

¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.77 (d, J=7.32 Hz, 3H) 1.47 (d, J=7.47Hz, 2H) 1.58-1.64 (m, 4H) 2.64 (br. S., 2H) 2.83 (dd, J=16.70, 7.47 Hz,2H) 3.52 (br. S., 2H) 3.83 (dd, J=11.21, 7.40 Hz, 1H) 5.92 (d, J=11.13Hz, 1H) 7.08 (d, J=8.20 Hz, 2H) 7.33 (dd, J=8.72, 2.27 Hz, 1 H) 7.46 (d,J=8.35 Hz, 2 H) 7.52 (d, J=2.20 Hz, 1H) 7.59 (d, J=8.79 Hz, 1H) 10.47(br. S., 1H)

MS (M+H)⁺: 535

Example 233 cis-1-(2,4-dichloropheenyl)-5-(4-fluorophenyl)-N-(hexahydrocyclopenta-[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride

¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.77 (d, J=7.32 Hz, 3H) 1.47 (d, J=8.64Hz, 2H) 1.55-1.67 (m, 4H) 2.63 (br. S., 2H) 2.81 (dd, J=15.16, 8.86 Hz,2H) 3.49 (br. S., 3H) 5.93 (d, J=1.28 Hz, 1H) 7.01-7.25 (m, 4H) 7.32(dd, J=8.72, 2.42 Hz, 1H) 7.51 (d, J=2.34 Hz, 1H) 7.60 (d, J=8.64 Hz,1H) 10.35 (br. S., 1H)

MS (M+H)⁺: 475

Example 96cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride

¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.78 (d, J=7.18 Hz, 3H) 1.58 (br. S.,4H) 1.76 (br. S., 4H) 3.32 (br. S, 4H) 3.85 (m, 1H) 5.95 (d, J=11.28 Hz,1H) 7.15 (d, J=8.50 Hz, 2H) 7.23-7.36 (m, 3H) 7.51 (d, J=2.34 Hz, 1H)7.61 (d, J=8.79 Hz, 1H) 10.89 (br. S., 1H)

MS (M+H)⁺: 479

Example 207cis-N-azepan-1-yl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride

¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.78 (d, J=7.18 Hz, 3H) 1.58 (br. S.,4H) 1.77 (br. S., 4H) 3.33 (br. S., 4H) 3.85 (dd, J=11.28, 7.18 Hz, 1H)5.94 (d, J=11.28 Hz, 1H) 7.08 (d, J=8.35 Hz, 2H) 7.34 (dd, J=8.72, 2.27Hz, 1H) 7.46 (d, J=8.35 Hz, 2H) 7.52 (d, J=2.34 Hz, 1H) 7.61 (d, J=8.64Hz, 1H) 10.98 (br. S., 1H)

MS (M+H)⁺: 523

Example 227cis-N-azepan-1-yl)-5-(4-fluorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride

¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.78 (d, J=7.32 Hz, 3H) 1.59 (br. S.,4H) 1.78 (br. S., 4H) 3.36 (br. S., 4H) 3.84 (dd, J=11.43, 7.32 Hz, 1H)5.96 (d, J=11.43 Hz, 1H) 6.99-7.21 (m, 4H) 7.33 (dd, J=8.79, 2.20 Hz,1H) 7.51 (d, J=2.34 Hz, 1H) 7.63 (d, J=8.79 Hz, 1H), 11.06 (br. S., 1H)

MS (M+H)⁺: 463

Example 271cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride

¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.80 (d, J=7.18 Hz, 3H) 1.59 (br. S.,4H) 1.79 (br. S., 4H) 3.38 (d, J=4.54 Hz, 4H) 3.66 (s, 3H) 3.80 (dd,J=11.28, 7.32 Hz, 1H) 5.89 (d, J=11.28 Hz, 1H) 6.78 (d, J=8.50 Hz, 2H)7.03 (d, J=8.50 Hz, 2H) 7.32 (dd, J=8.79, 2.34 Hz, 1H) 7.49 (d, J 2.34Hz, 1H) 7.63 (d, J=8.79 Hz, 1H) 11.12 (br. S., 1H)

MS (M+H)⁺: 475

Example 277cis-1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride

¹H NMR (300 MHz, CHLOROFORM-d) δ ppm 0.94 (d, J=7.32 Hz, 3H) 1.78 (m,6H) 3.03 (br. S., 2H) 3.74 (s, 3H) 3.66-3.88 (m, 3H) 3.99 (br. S., 2H)5.86 (d, J=11.86 Hz, 1H) 6.75 (d, J=8.50 Hz, 2H) 6.96 (d, J=8.50 Hz, 2H)7.12 (dd, J=8.64, 2.20 Hz, 1H) 7.25 (d, J=2.20 Hz, 1H) 7.33 (d, J=8.64Hz, 1H) 9.58 (br. S., 1H)

MS (M+H)⁺: 487

Example 343cis1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride

Example compound 277 (0.82 mmol) was dissolved in 10 mL dichloromethane.A solution of 1 M BBr₃ (5 eq.) in dichloromethane was added at 0° C. andthe reaction was stirred overnight at ambient temperature. The solidformed was filtered off and the solvent was evaporated. A solution of 2N HCl/diethyl ether was added to form the hydrochloride.

¹H NMR (300 MHz, METHANOL-d₄) δ ppm 0.95 (d, J=7.18 Hz, 3H) 1.65 (br.S., 2H) 1.79 (br. S., 4H) 2.95 (br. S., 2H) 3.11 (dd, J=16.48, 10.03 Hz,2H) 3.81 (dd, J=11.43, 7.18 Hz, 1H) 4.03 (m, 2H) 5.90 (d, J=11.43 Hz,1H) 6.64 (d, J8.06 Hz, 2H) 6.95 (d, J=8.06 Hz, 2H) 7.20 (m, 1H) 7.39 (d,J=2.20 Hz, 1H) 7.42 (d, J=8.79 Hz, 1H)

MS (M+H)⁺: 473

Example 92 (+)-cis-5-(4Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide hydrochloride

¹H NMR (400 MHz, METHANOL-d₄) δ ppm 0.94 (d, J=7.42 Hz, 3H) 1.68 (br,2H) 1.98 (dt, J=11.28, 5.59 Hz, 4H) 3.53 (br, 4H) 3.90 (td, J=11.53,7.42 Hz, 1H) 5.99 (d, J=11.53 Hz, 1H) 7.16 (d, J=8.40 Hz, 2H) 7.20-7.29(m, 3H) 7.36-7.48 (m, 2H)

[a]₅₈₉ ^(RT)=+131.73

Example 93(−)-cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide hydrochloride

¹H NMR (400 MHz, METHANOL-d₄) δ ppm 0.94 (d, J=7.42 Hz, 3H) 1.68 (br,2H) 1.98 (dt, J=11.28, 5.59 Hz, 4H) 3.53 (br, 4H) 3.90 (td, J=11.53,7.42 Hz, 1H) 5.99 (d, J=11.53 Hz, 1H) 7.16 (d, J=8.40 Hz, 2H) 7.20-7.29(m, 3H) 7.36-7.48 (m, 2H)

[a]₅₈₉ ^(RT)=−126.71

Example 379cis-5-(4chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamidehydrochloride

Phosphorous pentasulfide was added in portions (5×0.570 g, 12.9 mmol) toa solution of example compound 1 (6.46 mmol) in dry toluene (30 ml). Themixture was stirred and heated to reflux for 15 hours. The solid wasfiltered off and washed with dichloromethane. The solvent was evaporatedand a bright yellow solid was isolated, which was then treated withaqueous ammonium solution and extracted with ethyl acetate, dried overNa₂SO₄ and filtered off. The solid obtained after evaporation of thesolvent was dissolved in acetone and a solution of 2 N HCl in diethylether to form the corresponding hydrochloride. The pale yellow solidobtained by filtration was identified ascis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamidehydrochloride (85% yield).

¹H NMR (300 MHz, METHANOL-d₄) δ ppm 0.95 (d, J=7.32 Hz, 3H) 1.62-1.78(m, 2H) 2.00 (m, 4H) 3.60 (m, 4H) 3.99 (dd, J=10.84, 7.32 Hz, 1H) 5.91(d, J=10.84 Hz, 1H) 7.22 (d, J=8.79 Hz, 1H) 7.18-7.25 (m, 2H) 7.25-7.31(m, 2H) 7.40 (d, J=8.79 Hz, 1H) 7.45 (d, J=2.20 Hz, 1H)

MS (M+H)⁺: 481

Example 1cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide hydrochloride

Step 1: Preparation ofcis-5-(4-Chloro-phenyl)-1-(2,4dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid hydrazide

cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbonylchloride (5.40 mmol) was refluxed for 2 hours in ethanol (25 mL). Thereaction mixture was cooled to room temperature and 5 g of the hydrazinehydrate were added. The reaction mixture was heated to reflux for 4hours, cooled to room temperature and the solvent was removed in vacuum.The resulting residue was taken up in dichloromethane (30 mL) and washedwith water, dried and concentrated in vacuum. Chromatography with silicagel, eluting with Chloroform/Methanol system of appropriate polarity,yielded the title compound (65% yield) as a white solid.

Step 2:cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid(2,6-benzotriazlyl-piperidin-1-yl)amide

Benzotriazole (119 mg, 1 mmol),cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid hydrazide (0.5 mmol ), water (5 mL) and ethanol (5 mL) were stirredfor 10 min at room temperature. Glutaraldehyde (200 mg, 0.5 mMol, 25%aqueous solution) was slowly added to the reaction mixture, and stirringwas continued overnight at room temperature. The solvent was removed andthe insoluble products were filtered off, washed with water, and driedunder vacuum, yielding the title compound (66% yield) as a white solid.

Step 3:cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide

cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid(2,6-benzotriazlyl-piperidin-1-yl)amide (0.33mmol) intetrahydrofuran (10 mL) and sodium borohydride ( 38 mg, 1 mmol) werestirred at room temperature overnight . The reaction was quenched withwater, and the product was extracted with dichloromethane, washed withwater and dried. Solvent evaporation under reduced pressure led to thetitle compound. The product was purified by recrystallization fromethanol, yielding the title compound (41% yield) as a white solid.

The following examples were prepared using the methods described above.MS No STRUCTURE Name ¹H-NMR (M + H)⁺  1

cis-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide hydro-chloride 1H NMR (400 MHz, METHANOL-d₄) δppm 0.94(d, J=7.42Hz, 3H)1.68(br, 2H) 1.98(dt, J=11.28, 5.59Hz, 4H) 3.53(br, 4H) 3.90(td,J=11.53, 7.42Hz, 1H) 5.99(d, #J=11.53Hz, 1H) 7.16(d, J=8.40Hz, 2H)7.20-7.29(m, 3H) 7.36-7.48(m, 2H) 466  2

trans-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide hydro-chloride ¹H NMR (400 MHz, DMSO-d₆) δ ppm 1.38(d, J=7.03Hz, 3H) 1.42(m,2H) 1.71(m, 4H) 3.12(m, 4H) 3.42(dt, J=13.38, 5.86Hz, 1H) 5.36(d,J=5.86Hz, 1H) 7.19(d, #J=8.21Hz, 2H) 7.31(d, J=8.60Hz, 3H) 7.49(d,J=2.34Hz, 1H) 7.53(d, J=8.60Hz, 1H) 10.49(s, 1H) 466  3

cis-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid azepan-1-ylamide  4

trans-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid azepan-1-ylamide  5

cis-[5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-(4- cyclohexyl-piperazin-1-yl)- methanone 533 6

trans-[5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-(4- cyclohexyl-piperazin-1-yl)- methanone 533 7

cis-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid pyrrolidin-1-ylamide 451  8

trans-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid pyrrolidin-1-ylamide 451  9

cis-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid (4-methyl-piperidin-1-yl)-amide479  10

trans-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid (4-methyl-piperidin-1-yl)-amide479  11

cis-[5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-piperidin- 1-yl-methanone 450  12

trans-[5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-piperidin- 1-yl-methanone 450  13

cis-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid (hexahydro-cyclopenta[c]pyrrol-2-yl)-amide 491  14

trans-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid(hexahydro-cyclopenta-[c]pyrrol-2-yl)-amide 491  15

cis-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid (2,3-dihydro-indol-1-yl)-amide 499 16

trans-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid (2,3-dihydro-indol-1-yl)-amide 499 17

cis-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid cyclobutylamide 436  18

5-(4-Chloro-phenyl)-1-(2,4-dichloro- phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid cyclo- hexyl methyl-amide 478  19

cis-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-py-razole-3-carboxylic acid 1H NMR (400 MHz, CHLOROFORM-d)δppm 0.96(d, J=7.42Hz, 3H) 3.82(td, J=11.72, 7.42Hz, 1H) 5.91(d,J=11.72Hz, 1H) 7.04(d, J=8.60Hz, 2H) 7.11(dd, J=8.60, #2.34Hz, 1H)7.21-7.30(m, 4H) 384  20

trans-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-py-razole-3-carboxylic acid 1H NMR (400 MHz, CHLOROFORM-d)δppm 1.52(d, J=7.03Hz, 3H) 3.52(m, 1H) 5.39(d, J=5.47Hz, 1H) 7.08(ddd,J=13.92, 5.62, 5.28Hz, 3H) 7.14-7.34(m, 4H) 384  21

cis-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid 398  22

trans-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 398  23

cis-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-py-razole-3-carboxylic acid methyl ester 1H NMR (400 MHz,CHLOROFORM-d) δppm 0.94(d, J=7.32Hz, 3H) 3.80(td, J=11.48, 7.32Hz, 1H),3.88(s, 3H) 5.82(d, J=11.48Hz, 1H) 7.04(m, 2H) 7.10(dd, #J=8.67, 2.32Hz,1H) 7.20-7.24(m, 3H) 7.27(m, 1H) 398  24

trans-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-py-razole-3-carboxylic acid methyl ester 1H NMR (400 MHz,CHLOROFORM-d) δppm 1.49(d, J=7.32Hz, 3H) 3.50(td, J=7.32Hz, 5.60 1H)3.90(s, 3H) 5.35(d, J=5.60Hz, 1H) 7.04(m, 2H) 7.10(m, 1H) 7.20-7.27(m,4H) 398  25

cis-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-py-razole-3-carboxylic acid ethyl ester 411  26

trans-5-(4-Chloro-phenyl)-1-(2,4- dichloro-phenyl)-4-methyl-4,5-dihydro-1H-py-razole-3-carboxylic acid ethyl ester 411  27

5-(4-Chloro-phenyl-1-(2,4-dichloro- phenyl)-4-methyl-4,5-dihydro-1H-py-razole-3-carboxylic acid cyclo hexyl ester 465  28

5-(4-Chloro-phenyl)-1-(2,4-dichloro- phenyl)-4,4-dimethyl-4,5-dihydro-1-H-pyrazole-3-carboxylic acid 397  29

5-(4-Chloro-phenyl)-1-(2,4-dichloro- phenyl)-4,4-dimethyl-4,5-dihydro-1-H-pyrazole-3-carboxylic acid piperidin-1-ylamide 479  30

5-(4-Chloro-phenyl)-1-(2,4-dichloro- phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 519  31

5-(4-Chloro-phenyl)-1-(2,4-dichloro- phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylic acid 385  32

5-(4-Chloro-phenyl)-1-(2,4-dichloro- phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin- 1-ylamide 467  33

5-(4-Chloro-phenyl)-1-(2,4-dichloro- phenyl)-4-(2-hydroxy-ethyl)-4,5-di-hydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 495  34

5-(4-Chloro-phenyl)-1-(2,4-dichloro- phenyl)-4-(2-hydroxy-ethyl)-4,5-di-hydro-1H-pyrazole-3-carboxylic acid 413  35

5-(4-Chloro-phenyl)-1-(2,4-dichloro- phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 483  36

5-(4-Chloro-phenyl)-1-(2,4-dichloro- phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid 401  37

5-(4-Chloro-phenyl)-1-(2,4-dichloro- phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin- 1-ylamide 479  38

5-(4-Chloro-phenyl)-1-(2,4-dichloro- phenyl)-4-formyl-4,5-dihydro-1H-py-razole-3-carboxylic acid 397  39

5-(4-chlorophenyl)-4-cyano-1-(2,4- dichlorophenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3- carboxamide 476  40

5-(4-Chloro-phenyl)-4-cyano-1-(2,4- dichloro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic acid 394  41

1-(2,4-Dichloro-phenyl)-5-(4-fluoro- phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin- 1-ylamide 449  42

1-(2,4-Dichloro-phenyl)-4-ethyl-5- (4-fluoro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin- 1-ylamide 463  43

1-(2,4-Dichloro-phenyl)-5-(4-fluoro- phenyl)-4,4-dimethyl-4,5-dihydro-1-H-pyrazole-3-carboxylic acid piperidin-1-ylamide 463  44

1-(2,4-Dichloro-phenyl)-5-(4-fluoro- phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 503  45

1-(2,4-Dichloro-phenyl)-5-(4-fluoro- phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin- 1-ylamide 451  46

1-(2,4-Dichloro-phenyl)-5-(4-fluoro- phenyl)-4-(2-hydroxy-ethyl)-4,5-di-hydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 479  47

1-(2,4-Dichloro-phenyl)-4- fluoromethyl-5-(4-fluoro-phenyl)-4,5-dihydro-1H-pyrazole-3- carboxylic acid piperidin-1-ylamide 467  48

1-(2,4-Dichloro-phenyl)-5-(4-fluoro- phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin- 1-ylamide 463  49

4-Cyano-1-(2,4-dichloro-phenyl)-5- (4-fluoro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin- 1-ylamide 460  50

5-(4-Bromo-phenyl)-1-(2,4-dichloro- phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin- 1-ylamide 509  51

5-(4-Bromo-phenyl)-1-(2,4-dichloro- phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin- 1-ylamide 523  52

5-(4-Bromo-phenyl)-1-(2,4-dichloro- phenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 523  53

5-(4-Bromo-phenyl)-1-(2,4-dichloro- phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 563  54

5-(4-Bromo-phenyl)-1-(2,4-dichloro- phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin- 1-ylamide 511  55

5-(4-Bromo-phenyl)-1-(2,4-dichloro- phenyl)-4-(2-hydroxy-ethyl)-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 539  56

5-(4-Bromo-phenyl)-1-(2,4-dichloro- phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 527  57

5-(4-Bromo-phenyl)-1-(2,4-dichloro- phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin- 1-ylamide 523  58

5-(4-Bromo-phenyl)-4-cyano-1-(2,4- dichloro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin- 1-ylamide 520  59

cis-5-(5-Chloro-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 471  60

trans-5-(5-Chloro-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 471  61

cis-5-(5-Chloro-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 485  62

trans-5-(5-Chloro-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 485  63

5-(5-Chloro-thiophen-2-yl)-1-(2,4- dichloro-phenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 485  64

5-(5-Chloro-thiophen-2-yl)-1-(2,4- dichloro-phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3- carboxylic acid piperidin-1-ylamide 525  65

5-(5-Chloro-thiophen-2-yl)-1-(2,4- dichloro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 473  66

5-(5-Chloro-thiophen-2-yl)-1-(2,4- dichloro-phenyl)-4-(2-hydroxy-ethyl)-4,5-dihydro-1H-pyrazole-3- carboxylic acid piperidin-1-ylamide501  67

5-(5-Chloro-thiophen-2-yl)-1-(2,4- dichloro-phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 489  68

5-(5-Chloro-thiophen-2-yl)-1-(2,4- dichloro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 485  69

5-(5-Chloro-thiophen-2-yl)-4-cyano- 1-(2,4-dichloro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 482  70

cis-5-(5-Bromo-thiophen-2-yl)-1- 2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 515  71

trans-5-(5-Bromo-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 515  72

cis-5-(5-Bromo-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 529  73

trans-5-(5-Bromo-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 529  74

5-(5-Bromo-thiophen-2-yl)-1-(2,4-di- chloro-phenyl)-4,4-dimethyl-4,5-di-hydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 529  75

cis-5-(4-Bromo-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 515  76

trans-5-(4-Bromo-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 515  77

cis-5-(4-Bromo-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 529  78

trans-5-(4-Bromo-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 529  79

5-(4-Bromo-thiophen-2-yl)-1-(2,4- dichloro-phenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 529  80

5-(5-Bromo-thiophen-2-yl)-1-(2,4- dichloro-phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3- carboxylic acid piperidin-1-ylamide 569  81

5-(5-Bromo-thiophen-2-yl)-1-(2,4- dichloro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 517  82

5-(5-Bromo-thiophen-2-yl)-1-(2,4- dichloro-phenyl)-4-(2-hydroxy-ethyl)-4,5-dihydro-1H-pyrazole-3- carboxylic acid piperidin-1-ylamide 545  83

5-(5-Bromo-thiophen-2-yl)-1-(2,4- dichloro-phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 533  84

5-(5-Bromo-thiophen-2-yl)-1-(2,4- dichloro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 529  85

5-(5-Bromo-thiophen-2-yl)-4-cyano- 1-(2,4-dichloro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide 526  86

cis-5-(5-Chloro-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid 389  87

trans-[5-(5-Chloro-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-piperidin- 1-yl-methanone 389  88

cis-5-(5-Bromo-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid 433  89

trans-5-(5-Bromo-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid 433  90

cis-5-(4-Bromo-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid 433  91

trans-5-(4-Bromo-thiophen-2-yl)-1- (2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid 433 446

cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide N-oxide 480 447

cis-5-(4-chlorophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide N-oxide 446 448

cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide N-oxide 494 449

cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide N-oxide 460 450

cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide N-oxide 476 451

cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide N-oxide 442  92(+)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride  93(−)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride  94cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide 95trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide 96cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid azepan-1-ylamide hydrochloride  97trans-5-(4-Chlorophenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid azepan-1-ylamide hydrochloride  98cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide 99trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide100cis-5-(4-chlorophenyl)-N-(4-cyclopentylpiperazin-1-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 101cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-morpholino-4,5-dihydro-1H-pyrazole-3-carboxamide102cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(4-methylpiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide103cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(2,6-dimethylpiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide104cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (1,3-dioxo-1H,3H-benzo[de]isoquinolin- 2-yl)-amide 105cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (1H,3H-benzo[de]isoquinolin-2-yl)-amide 106cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-( ® -2-(methoxymethyl)pyrrolidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 107cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((S)-2-(methoxymethyl)pyrrolidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 108cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (hexahydrocyclopenta[c]pyrrol-2-yl)-amide hydrochloride 109cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide110trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide111cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide112trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide113cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(2-methylindolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide114cis-5-(4-chlorophenyl)-N-(cyclohexylmethyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide115cis-5-(4-chlorophenyl)-N-(cycloheptylmethyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide116cis-5-(4-chlorophenyl)-N-cyclododecyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide117cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide118cis-N-(4-tert-butylcyclohexyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide 119cis-5-(4-chlorophenyl)-N-cyclooctyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide120cis-N-(azocan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide121cis-N-(azocan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide122cis-azocan-1-yl(cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl)methanone123cis-5-(4-chlorophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide124cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-cycloheptyl-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide125trans-5-(4-chlorophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide126trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-cycloheptyl-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide127cis-5-(4-chlorophenyl)-N-(cyclohexylmethyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide128(+)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide129(−)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide130(−)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1R,2R)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide131(+)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1R,2R)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide132(+)-cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide133(−)-cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide134cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(4-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide135cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(4-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide136cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(3-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide137cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(3-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide138cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(2-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide139cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(2-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide140cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(4-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide141cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(4-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide142cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(3-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide143cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(3-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide144cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(3,4-dihydropyridin-1(2H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide 145cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(3,4-dihydropyridin-1(2H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide146cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(5,6-dihydropyridin-1(2H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide147cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(5,6-dihydropyridin-1(2H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide148cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 149trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 150cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-py-razole-3-carboxylicacid cyclohexyl ester 151N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxamide1521-(2-chlorophenyl)-5-(4-chlorophenyl)-4,4-dimethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide153N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxamide154cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide 155trans-5-(4-Chloro-phenyl)-1-(2,4-dichlorophenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide 156cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide157trans-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide158cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide159 trans1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide1605-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-(piperidin-1-ylcarbamoyl)-4,5-dihydro-1H-pyrazole-4-carboxylicacid 1615-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,4-difluoro-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide162cis-5-(4-chlorophenyl)-4-cyano-1-(2,4-dichlorophenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide163cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-4-cyano-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide164cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-cyano-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide165cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-cyano-4,5-dihydro-1H-pyrazole-3-carboxamide166trans-5-(4-chlorophenyl)-4-cyano-1-(2,4-dichlorophenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide167trans-N-(azepan-1-yl)-5-(4-chlorophenyl)-4-cyano-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide168trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-cyano-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide169cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 170trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 171cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide172trans-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide173cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide174trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide175cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide176trans-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide177cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide178trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide179cis-5-(4-chlorophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide180cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-cycloheptyl-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide181cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide182cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide183cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(indolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide184cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-N-(indolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide185cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 186trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 187cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide188trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide189cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide190trans-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide191cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide192cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide193cis-5-(4-bromophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide194cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-cycloheptyl-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide195cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide196cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide197cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(indolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide198cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-N-(indolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide199cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 200trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 201cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 202trans-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 203cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide204trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide205 cis5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide206trans-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide207cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 208trans-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 209cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide210cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide211cis-5-(4-bromophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide212cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-cycloheptyl-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide213cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 214cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide215cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide216cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide217(+)-cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide218(−)-cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide219(+)-cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide220(−)-cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide221cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 222trans-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 223cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide224trans-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide225cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide226trans-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide227cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 228trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 229cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide230trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide231cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide232cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide233cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 234cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide235cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide236cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide237(+)-cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide238(−)-cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide239(+)-cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide240(−)-cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide241cis-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 242trans-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 243cis-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide244trans-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide245cis-1-(2-chlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide246trans-1-(2-chlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide247cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide248trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide249cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide250trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide251cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide252cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide253cis-1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide254cis-1-(2-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide255cis-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide256cis-1-(2-chlorophenyl)-N-(indolin-1-yl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide257(+)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide258(−)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide259(+)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide260(−)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide261cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 262trans-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 263cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 264trans-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 265cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 266(+)-cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 267(−)-cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 268trans-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide269cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide270trans-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide271cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 272trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 273cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide274trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide275cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide276cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide277cis-1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 278cis-1-(2-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide279cis-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide280cis-1-(2-chlorophenyl)-N-(indolin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide281(+)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide282(−)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide283(+)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide284(−)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide285cis-1-(2,4-dichlorophenyl)-N-(4-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide286cis-1-(2-chlorophenyl)-N-(4-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide287cis-1-(2,4-dichlorophenyl)-N-(3-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide288cis-1-(2-chlorophenyl)-N-(3-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide289cis-1-(2,4-dichlorophenyl)-N-(2-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide290cis-1-(2-chlorophenyl)-N-(2-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide291cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(4-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide292cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(4-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide293cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(3-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide294cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(3-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide295cis-1-(2,4-dichlorophenyl)-N-(3,4-dihydropyridin-1(2H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide296cis-1-(2-chlorophenyl)-N-(3,4-dihydropyridin-1(2H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide297cis-1-(2,4-dichlorophenyl)-N-(5,6-dihydropyridin-1(2H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide298cis-1-(2-chlorophenyl)-N-(5,6-dihydropyridin-1(2H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide299cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide300trans-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide301cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide302trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide303cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide304trans-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide3051-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4,4-dimethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide306N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxamide3071-(2-chlorophenyl)-5-(4-methoxyphenyl)-4,4-dimethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3081-(2,4-dichlorophenyl)-4-formyl-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3091-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-3-(piperidin-1-ylcarbamoyl)-4,5-dihydro-1H-pyrazole-4-carboxylicacid 3101-(2,4-dichlorophenyl)-4-(2-hydroxyethyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3111-(2,4-dichlorophenyl)-4-(fluoromethyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide312cis-4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide313trans-4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide314cis-N-(azepan-1-yl)-4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide315trans-N-(azepan-1-yl)-4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide316cis-1-(2-chlorophenyl)-4-cyano-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide317trans-1-(2-chlorophenyl)-4-cyano-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3181-(2,4-dichlorophenyl)-4-hydroxy-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3191-(2-chlorophenyl)-4,4-difluoro-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-~1H-pyrazole-3-carboxamide3201-(2-chlorophenyl)-4-formyl-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3211-(2-chlorophenyl)-5-(4-methoxyphenyl)-3-(piperidin-1-ylcarbamoyl)-4,5-dihydro-1H-pyrazole-4-carboxylicacid 3221-(2-chlorophenyl)-4-(2-hydroxyethyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3231-(2-chlorophenyl)-4-(fluoromethyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3241-(2-chlorophenyl)-4-hydroxy-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide325cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide326trans-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide327cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide328trans-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide329cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide330trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide331cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide332trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide333cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide334cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide335cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide336cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide337cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide338cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide339(+)-cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide340(−)-cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide341(+)-cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide342(−)-cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide343cis-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide344trans-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide345cis-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide346trans-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide347cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide348trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide349cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide350trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide351cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide352cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide353cis-1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 354cis-1-(2-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide355cis-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide356cis-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide357(+)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide358(−)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide359(+)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide360(−)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide361cis-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 362trans-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 363cis-1-(2-chlorophenyl)-5-(5-chlorothiophen-2-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 364trans-1-(2-chlorophenyl)-5-(5-chlorothiophen-2-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 365cis-5-(5-bromothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 366trans-5-(5-bromothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 367cis-1-(2,4-dichlorophenyl)-4-methyl-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid 368trans-1-(2,4-dichlorophenyl)-4-methyl-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid 369cis-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide370trans-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide371cis-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide372trans-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide373cis-1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 374trans-1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 375cis-1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide376trans-1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide377cis-1-(2-chlorophenyl)-4-methyl-5-phenyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide378trans-1-(2-chlorophenyl)-4-methyl-5-phenyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide379cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamidehydrochloride 380trans-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4~5-dihydro-1H-pyrazole-3-carbothioamide381cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide382trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide383cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbothioamide384cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbothioamide385cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide386trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide387cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide388trans-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide389cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide390trans-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide391cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide392trans-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide393cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide394cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbothioamide395trans-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide396cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide397cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbothioamide398trans-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide399cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide400trans-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide401cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide402trans-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide403cis-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide404trans-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide405cis-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide406trans-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide4077-(4-Chloro-phenyl)-6-(2,4-dichlorophenyl)-5,6-diaza-spiro[2,4]hept-4-ene-4-carboxylicacid piperidin-1-ylamide 4086-(2,4-Dichloro-phenyl)-7-(4-methoxy-phenyl)-5,6-diaza-spiro[2,4]hept-4-ene-4-carboxylicacid piperidin-1-ylamide 409(+)-cis-N-((1S,2S)-2-(benzyloxy)cyclohexyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide[410]cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide[411]cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide[412](4R,5S)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [413]cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [414]cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide415cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide416 trans-ethyl5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxylate417cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 418cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 419(−)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide420(+)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide421 trans-ethyl1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylate422cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-((1R,2S,4R)-1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide 423cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(3-methylcyclohexyl)-4,5-dihydro-1H-pyrazole-3-carboxamide424cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(2-methylcyclohexyl)-4,5-dihydro-1H-pyrazole-3-carboxamide426trans-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 427cis-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 428cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride [429]1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [430]cis-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride [431]trans-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide432cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide434cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide436(+)-cis-N-((1S,2S)-2-(benzyloxy)cyclohexyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide437(−)-cis-N-((1R,2R)-2-(benzyloxy)cyclohexyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide438cis-N-(azocan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide439cis-N-(azocan-1-yl)-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide440cis-N-(azocan-1-yl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide441cis-N-(azocan-1-yl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide442cis-N-(azocan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide443cis-N-(azocan-l-yl)-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide444(+)-cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid azepan-1-ylamide hydrochloride 445(−)-cis-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid azepan-1-ylamide hydrochloridePharmacological Data

The binding of the the pyrazoline compounds of general formula I toCB1-receptors was determined according to the method described in thesection Pharmacological Methods, Part I.

The pyrazoline compounds of the present invention show a high affinityto the CB1-receptor (table 1.) TABLE 1 Compound according InhibitionInhibition to example IC₅₀. [nM] [%, 10⁻⁷ M] [10⁻⁸, M] 5 199.5 7 41 20.79 77.3 13 25.1 70.6 27.6 15 100 19 −3.6 −0.7 21 23 11 71 >1000 75 180 967.9 80 65 100 32.6 5.4 101 34.9 27.7 103 60.6 55.3 19.5 104 31.7 −0.4105 31.4 35.9 106 39 20.4 107 43.9 2.7 108 31.6 113 128.1 55.5 24.7 11428.3 −13 119 51.4 73.7 19.5 120 75.5 37 123 31.9 90.8 39.9 128 35.3 18.0129 69 72.3 11.6 200 −11.2 3 207 71 73 48.3 211 30 69.8 37.2 213 53 221−6.3 −2.2 227 122 65.3 15.3 231 112 50.5 23.2 233 43.9 27.9 235 25.9 5.4261 −6.9 −5 265 60 62 29.2 271 61 73.5 30.6 275 66 69.1 26.1 277 20 61.617.9 279 19 62.4 14.7 281 39.0 10.2 282 44.3 9.6 343 −10.1 −15.8 344−23.3 −27.3 363 11.3 12.2 367 11 7.2 375 140 376 70.8 379 111.7 74.527.0 409 −5.8 −37 410 82 58.1 42.4 412 −15.4 −11.1 413 17.3 13.8 41436.2 28.7 415 79.3 32.3 416 182 93.5 41 417 38.5 14.8 418 36 62.6 19.9419 54.3 57.1 27.8 420 30.4 2.8 421 31.2 38 422 −2 −8.4 423 45.5 66.733.1 424 29.7 65.7 39.3 425 66.8 30.7 426 280 427 160 428 42.6 28.4 429−11 −10.1 430 >1000 431 79 432 89 433 >1000 434 89 435 199.5 437 40.914.7

The antagonism of the pyrazoline compounds of general formula I to theCB1-receptor was determined according to the method described inPharmacological methods, part V (table 2). TABLE 2 Compound according toexample Antagonism [%] 19 −18 70 81 93 97 376 75 375 58 430 23 431 72432 89 433 57 435 40

1. A 4-substituted pyrazoline compound of general formula I,

wherein X is O or S; R¹ and R², independently of one another, in eachcase represent an unsubstituted or at least mono-substituted aryl orheteroaryl radical, which may be condensed with an unsubstituted or atleast mono-substituted mono- or polycyclic ring system; or a saturatedor unsaturated, unsubstituted or at least mono-substituted, optionallyat least one heteroatom as a ring member containing cycloaliphaticradical, which may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bridgedby at least one unsubstituted or at least mono-substituted alkylenegroup; R³ an unsubstituted or at least mono-substituted aryl orheteroaryl radical, which may be condensed with an unsubstituted or atleast mono-substituted mono- or polycyclic ring system; a saturated orunsaturated, unsubstituted or at least mono-substituted, optionally atleast one heteroatom as a ring member containing cycloaliphatic radical,which may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bridgedby at least one unsubstituted or at least mono-substituted alkylenegroup; a saturated or unsaturated, unsubstituted or at leastmono-substituted, optionally at least one heteroatom as a ring membercontaining cycloaliphatic radical which together with a saturated orunsaturated, unsubstituted or at least mono-substituted, optionally atleast one heteroatom as a ring member containing cycloaliphatic radicalforms a saturated or unsaturated, unsubstituted or at leastmono-substituted, optionally at least one heteroatom as a ring membercontaining spirocyclic residue via a common ring atom; a —O—R⁶ moiety; a—NR⁷R⁸ moiety or a —NR⁹—O—R¹⁰ moiety; R⁴ represents F; Cl; Br; I; —CN;—NO₂; —NC; —OH; —NH₂; —SH; —C(═O)—H; —C(═O)—OH; —C(═O)—OR¹⁷; a saturatedor unsaturated, unsubstituted or at least mono-substituted aliphaticradical; a saturated or unsaturated, unsubstituted or at leastmono-substituted, optionally at least one heteroatom as a ring membercontaining cycloaliphatic radical, which may be condensed with anunsubstituted or at least mono-substituted mono- or polycyclic ringsystem and/or may be bonded via an unsubstituted or at leastmono-substituted alkylene group, alkenylene group or alkinylene groupand/or may be bridged by at least one unsubstituted or at leastmono-substituted alkylene group: an unsubstituted or at leastmono-substituted aryl or heteroaryl radical, which may be condensed withan unsubstituted or at least mono-substituted mono- or polycyclic ringsystem and/or may be bonded via an optionally at least mono-substitutedalkylene group, alkenylene group or alkinylene group; a —O—R¹¹ moiety; a—S—R¹² moiety; a —NH—R¹³ moiety or a —NR¹⁴R¹⁵ moiety; R⁵ represents H;F; Cl; Br; I; —CN; —NO₂; —NC; —OH; —NH₂; —SH; —C(═O)—H; —C(═O)—OH;—C(═O)—OR¹⁷; a saturated or unsaturated, unsubstituted or at leastmono-substituted aliphatic radical; a saturated or unsaturated,unsubstituted or at least mono-substituted, optionally at least oneheteroatom as a ring member containing cycloaliphatic radical, which maybe condensed with an unsubstituted or at least mono-substituted mono- orpolycyclic ring system and/or may be bonded via an unsubstituted or atleast mono-substituted alkylene group, alkenylene group or alkinylenegroup and/or may be bridged by at least one unsubstituted or at leastmono-substituted alkylene group; an unsubstituted or at leastmono-substituted aryl or heteroaryl radical, which may be condensed withan unsubstituted or at least mono-substituted mono- or polycyclic ringsystem and/or may be bonded via an unsubstituted or at leastmono-substituted alkylene group, alkenylene group or alkinylene group; a—O—R¹¹ moiety; a —S—R¹² moiety; a —NH—R¹³ moiety or a —NR¹⁴R¹⁵ moiety;or R⁴ and R⁵ together with the bridging carbon atom form a saturated orunsaturated, unsubstituted or at least mono-substituted, optionally atleast one heteroatom as a ring member containing cycloaliphatic radical;R⁶ represents a hydrogen atom; a saturated or unsaturated, unsubstitutedor at least mono-substituted aliphatic radical; a saturated orunsaturated, unsubstituted or at least mono-substituted, optionally atleast one heteroatom as a ring member containing cycloaliphatic radical,which may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bondedvia an unsubstituted or at least mono-substituted alkylene group,alkenylene group or alkinylene group and/or may be bridged by at leastone unsubstituted or at least mono-substituted alkylene group; anunsubstituted or at least mono-substituted aryl or heteroaryl radical,which may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bondedvia an unsubstituted or at least mono-substituted alkylene group,alkenylene group or alkinylene group; a —P(═O)(OR¹⁶)₂ moiety; a—C(═O)—OR¹⁷ moiety; a —C(═O)—NH—R¹⁸ moiety or a —C(═O)—R¹⁹ moiety; R⁷and R⁸, independently of one another, in each case represent a hydrogenatom; a saturated or unsaturated, unsubstituted or at leastmono-substituted aliphatic radical; a saturated or unsaturated,unsubstituted or at least mono-substituted, optionally at least oneheteroatom as a ring member containing cycloaliphatic radical, which maybe condensed with an unsubstituted or at least mono-substituted mono- orpolycyclic ring system and/or may be bonded via an unsubstituted or atleast mono-substituted alkylene group, alkenylene group or alkinylenegroup and/or may be bridged by at least one unsubstituted or at leastmono-substituted alkylene group; a saturated or unsaturated,unsubstituted or at least mono-substituted, optionally at least oneheteroatom as a ring member containing cycloaliphatic radical whichtogether with a saturated or unsaturated, unsubstituted or at leastmono-substituted, optionally at least one heteroatom as a ring membercontaining cycloaliphatic radical forms a saturated or unsaturated,unsubstituted or at least mono-substituted, optionally at least oneheteroatom as a ring member containing spirocyclic residue via a commonring atom; an unsubstituted or at least mono-substituted aryl orheteroaryl radical, which may be condensed with an unsubstituted or atleast mono-substituted mono- or polycyclic ring system and/or may bebonded via an unsubstituted or at least mono-substituted alkylene group,alkenylene group or alkinylene group; a —P(═O)(OR¹⁶)₂ moiety; a—C(═O)—OR¹⁷ moiety; a —C(═O)—NH—R¹⁸ moiety; a —C(═O)—R¹⁹ moiety; a—S(═O)₂—R²⁰ moiety; or a —NR²¹R²² moiety; R⁹ represents hydrogen or asaturated or unsaturated, unsubstituted or at least mono-substitutedaliphatic radical; R¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R20, independentlyof one another, in each case represent a saturated or unsaturated,unsubstituted or at least mono-substituted aliphatic radical; asaturated or unsaturated, unsubstituted or at least mono-substituted,optionally at least one heteroatorn as a ring member containingcycloaliphatic radical, which may be condensed with an unsubstituted orat least mono-substituted mono- or polycyclic ring system and/or may bebonded via an unsubstituted or at least mono-substituted alkylene group,alkenylene group or alkinylene group and/or may be bridged by at leastone unsubstituted or at least mono-substituted alkylene group; or anunsubstituted or at least mono-substituted aryl or heteroaryl radical,which may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bondedvia an unsubstituted or at least mono-substituted alkylene group,alkenylene group or alkinylene group; R¹⁶, R¹⁷, R¹⁸ and R¹⁹,independently of one another, in each case represent a saturated orunsaturated, unsubstituted or at least mono-substituted aliphaticradical, or an unsubstituted or at least mono-substituted aryl orheteroaryl radical, which may be condensed with an unsubstituted or atleast mono-substituted mono- or polycyclic ring system and/or m ay bebonded via an unsubstituted or at least mono-substituted alkylene group,alkenylene group or alkinylene group; and R²¹ and R²², independently ofone another, in each case represent a hydrogen atom; a saturated orunsaturated, unsubstituted or at least mono-substituted aliphaticradical; a saturated or unsaturated, unsubstituted or at leastmono-substituted, optionally at least one heteroatom as a ring membercontaining cycloaliphatic radical, which may be condensed with anunsubstituted or at least mono-substituted mono- or polycyclic ringsystem and/or may be bonded via an unsubstituted or at leastmono-substituted alkylene group, alkenylene group or alkinylene group; asaturated or unsaturated, unsubstituted or at least mono-substituted,optionally at least one heteroatom as a ring member containingcycloaliphatic radical which together with a saturated or unsaturated,unsubstituted or at least monosubstituted, optionally at least oneheteroatom as a ring member containing cycloaliphatic radical forms asaturated or unsaturated, unsubstituted or at least mono-substituted,optionally at least one heteroatom as a ring member containingspirocyclic residue via a common ring atom; or an unsubstituted or atleast mono-substituted aryl or heteroaryl radical, which may becondensed with an unsubstituted or at least mono-substituted mono- orpolycyclic ring system and/or may be bonded via an unsubstituted or atleast mono-substituted alkylene group, alkenylene group or alkinylenegroup; whereby the following compounds are excluded [A] ethyl4,5-dimorpholino-1-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylate, [B]methyl1-phenyl-4,5-di(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxylate,[C]1-(4-chlorophenyl)-4-(hydroxymethyl)-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid, [D] ethyl5-morpholino-1,4-diphenyl-4,5-dihydro-1H-pyrazole-3-carboxylate, [E]ethyl4-(4-chlorophenyl)-1-(4-fluorophenyl)-5-morpholino-4,5-dihydro-1H-pyrazole-3-carboxylate,[F] ethyl1-(4-fluorophenyl)-5-morpholino-4-p-tolyl-4,5-dihydro-1H-pyrazole-3-carboxylate,[G] methyl4-(hydroxymethyl)-1-(2-(methoxycarbonyl)phenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylate,[H]benzofuran-2-yl(5-(4-hydroxyphenyl)-4-nitro-1-(3-phenyl-1H-pyrazol-5-yl)-4,5-dihydro-1H-pyrazol-3-yl)methanone,[I](5-(benzo[d][1,3]dioxol-5-yl)-4-nitro-1-(3-phenyl-1H-pyrazol-5-yl)-4,5-dihydro-1H-pyrazol-3-yl)(benzofuran-2-yl)methanone,[J]3-(benzofuran-2-carbonyl)-5-phenyl-1-(3-phenyl-1H-pyrazol-5-yl)-1H-pyrazole-4,4(5H)-dicarbonitrile,[K](5-(benzo[d][1,3]didxol-4-yl)-4-nitro-1-(3-phenyl-1H-pyrazol-5-yl)-4,5-dihydro-1H-pyrazol-3-yl)(benzofuran-2-yl)methanone,[L] ethyl1-(3-methoxypheyl)-5-morpholino-4-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylate,[M] ethyl1-(3-methoxyphenyl)-4-phenyl-5-(piperazin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxylate,which is optionally bonded to copolystyrol, [N]1-(3-methoxyphenyl)-4-phenyl-5-(piperazin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid, which is optionally bonded to copolystyrol and [O] ethyl5-(4-oxo-2,3-diphenyl-4,5-dihydro-2H-pyrazolo[4,3-d]pyridazin-7-yl)-1,4-diphenyl-4,5-dihydro-1H-pyrazole-3-carboxylate,optionally in form of one of its stereoisomers, preferably enantiomersor diastereomers, a racemate or in form of a mixture of at least two ofits stereoisomers, preferably enantiomers and/or diastereomers, in anymixing ratio, or a corresponding N-oxide thereof, or a physiologicallyacceptable salt thereof, or a corresponding solvate thereof.
 2. Acompound according to claim 1, characterized in that X is O or S; R¹ andR², independently of one another, in each case represent anunsubstituted or at least mono-substituted 6- or 10-membered arylradical, which may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system; an unsubstituted or atleast mono-substituted 5- to 14-membered heteroaryl radical, which maybe condensed with an unsubstituted or at least mono-substituted mono- orpolycyclic ring system; an unsubstituted or at least mono-substitutedC₃₋₁₆ cycloalkyl radical or C₄₋₁₆ cycloalkenyl radical, which in eachcase may be condensed with an unsubstituted or at least mono-substitutedmono- or polycyclic ring system and/or may be bridged by at least oneunsubstituted or at least mono-substituted C₁₋₅ alkylene group; or anunsubstituted or at least mono-substituted C₄₋₁₆ heterocycloalkylradical or C₅₋₁₆ heterocycloalkenyl radical, which in each case may becondensed with an unsubstituted or at least mono-substituted mono- orpolycyclic ring system and/or may be bridged by at least oneunsubstituted or at least mono-substituted C₁₋₅ alkylene group; R³represents an unsubstituted or at least mono-substituted 6- or10-membered aryl radical, which may be condensed with an unsubstitutedor at least mono-substituted mono- or polycyclic ring system; anunsubstituted or at least mono-substituted 5- to 14-membered heteroarylradical, which may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system; an unsubstituted or atleast mono-substituted C₃₋₁₆ cycloalkyl radical or C₄₋₁₆ cycloalkenylradical, which in each case may be condensed with an unsubstituted or atleast mono-substituted mono- or polycyclic ring system and/or may bebridged by at least one unsubstituted or at least mono-substituted C₁₋₅alkylene group; an unsubstituted or at least mono-substituted C₄₋₁₆heterocycloalkyl radical or C₅₋₁₆ heterocycloalkenyl radical, which ineach case may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bridgedby at least one unsubstituted or at least mono-substituted C₁₋₅ alkylenegroup, an unsubstituted or at least mono-substituted C₃₋₁₆ cycloalkylradical, C₄₋₁₆ cycloalkenyl radical, C₄₋₁₆ heterocycloalkyl radical orC₅₋₁₆ heterocycloalkenyl radical which together with an unsubstituted orat least mono-substituted C₃₋₁₆ cycloalkyl radical, C₄₋₁₆ cycloalkenylradical, C₄₋₁₆ heterocycloalkyl radical or C₅₋₁₆ heterocycloalkenylradical forms an unsubstituted or at least mono-substituted spirocyclicresidue via a common ring atom; a —O—R⁶ moiety; a —NR⁷R⁸ moiety or a—NR⁹—O—R¹⁰ moiety; R⁴ represents F; Cl; Br; I; —CN; —NO₂; —NC; —OH;—NH₂; —SH; —C(═O)—H; —C(═O)—OH; —C(═O)—OR¹⁷; an unsubstituted or atleast mono-substituted C₁₋₁₆ alkyl radical, C₂₋₁₆ alkenyl radical orC₂₋₁₆ alkinyl radical; an unsubstituted or at least mono-substitutedC₃₋₁₆ cycloalkyl radical or C₄₋₁₆ cycloalkenyl radical, which in eachcase may be condensed with an unsubstituted or at least mono-substitutedmono- or polycyclic ring system and/or may be bonded via anunsubstituted or at least mono-substituted C₁₋₅ alkylene group, C₂₋₅alkenylene group or C₂₋₅ alkinylene group and/or may be bridged by atleast one unsubstituted or at least mono-substituted C₁₋₅ alkylenegroup; an unsubstituted or at least mono-substituted C₄₋₁₆heterocycloalkyl radical or C₅₋₁₆ heterocycloalkenyl radical, which ineach case may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bondedvia an unsubstituted or at least mono-substituted C₁₋₅ alkylene group,C₂₋₅ alkenylene group or C₂₋₅ alkinylene group and/or may be bridged byat least one unsubstituted or at least mono-substituted C₁₋₅ alkylenegroup; an unsubstituted or at least mono-substituted 6- or 10-memberedaryl radical, which may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bondedvia an unsubstituted or at least mono-substituted C₁₋₅ alkylene group,C₂₋₅ alkenylene group or C₂₋₅ alkinylene group; or an unsubstituted orat least mono-substituted 5- to 14-membered heteroaryl radical, whichmay be condensed with an unsubstituted or at least mono-substitutedmono- or polycyclic ring system and/or may be bonded via anunsubstituted or at least mono-substituted C₁₋₅ alkylene group, C₂₋₅alkenylene group or C₂₋₅ alkinylene group; a —O—R¹¹ moiety; a —S—R¹²moiety; a —NH—R¹³ moiety or a —NR¹⁴R¹⁵ moiety; R⁵ represents H; F; Cl;Br; I; —CN; —NO₂; —NC; —OH; —NH₂; —SH; —C(═O)—H; —C(═O)—OH; —C(═O)—OR¹⁷;an unsubstituted or at least mono-substituted C₁₋₁₆ alkyl radical, C₂₋₁₆alkenyl radical or C₂₋₁₆ alkinyl radical; an unsubstituted or at leastmono-substituted C₃₋₁₆ cycloalkyl radical or C₄₋₁₆ cycloalkenyl radical,which in each case may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bondedvia an unsubstituted or at least mono-substituted C₁₋₅ alkylene group,C₂₋₅ alkenylene group or C₂₋₅ alkinylene group and/or may be bridged byat least one unsubstituted or at least mono-substituted C₁₋₅ alkylenegroup; an unsubstituted or at least mono-substituted C₄₋₁₆heterocycloalkyl radical or C₅₋₁₆ heterocycloalkenyl radical, which ineach case may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bondedvia an unsubstituted or at least mono-substituted C₁₋₅ alkylene group,C₂₋₅ alkenylene group or C₂₋₅ alkinylene group and/or may be bridged byat least one unsubstituted or at least mono-substituted C₁₋₅ alkylenegroup; an unsubstituted or at least mono-substituted 6- or 10-memberedaryl radical, which may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bondedvia an unsubstituted or at least mono-substituted C₁₋₅ alkylene group,C₂₋₅ alkenylene group or C₂₋₅ alkinylene group; or an unsubstituted orat least mono-substituted 5- to 14-membered heteroaryl radical, whichmay be condensed with an unsubstituted or at least mono-substitutedmono- or polycyclic ring system and/or may be bonded via anunsubstituted or at least mono-substituted C₁₋₅ alkylene group, C₂₋₅alkenylene group or C₂₋₅ alkinylene group; —O—R¹¹ moiety; a —S—R¹²moiety; a —NH—R¹³ moiety or a —NR¹⁴R¹⁵ moiety; or R⁴ and R⁵ togetherwith the bridging carbon atom form an unsubstituted or at leastmono-substituted C₃₋₁₆ cycloalkyl radical or C₄₋₁₆ cycloalkenyl radical;R⁶ represents a hydrogen atom; an unsubstituted or at leastmono-substituted C₁₋₁₆ alkyl radical, C₂₋₁₆ alkenyl radical or C₂₋₁₆alkinyl radical; an unsubstituted or at least mono-substituted C₃₋₁₆cycloalkyl radical or C₄₋₁₆ cycloalkenyl radical, which in each case maybe condensed with an unsubstituted or at least mono-substituted mono- orpolycyclic ring system and/or may be bridged by at least oneunsubstituted or at least mono-substituted C₁₋₅ alkylene group and/ormay be bonded via an unsubstituted or at least mono-substituted C₁₋₅alkylene group, C₂₋₅ alkenylene group or C₂₋₅ alkinylene group; anunsubstituted or at least mono-substituted C₄₋₁₆ heterocycloalkylradical or C₅₋₁₆ heterocycloalkenyl radical, which in each case may becondensed with an unsubstituted or at least mono-substituted mono- orpolycyclic ring system and/or may be bridged by at least oneunsubstituted or at least mono-substituted C₁₋₅ alkylene group and/ormay be bonded via an unsubstituted or at least mono-substituted C₁₋₅alkylene group, C₂₋₅ alkenylene group or C₂₋₅ alkinylene group; anunsubstituted or at least mono-substituted 6- or 10-membered arylradical, which may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bondedvia an unsubstituted or at least mono-substituted C₁₋₅ alkylene group,C₂₋₅ alkenylene group or C₂₋₅ alkinylene group; an unsubstituted or atleast mono-substituted 5- to 14-membered heteroaryl radical, which maybe condensed with an unsubstituted or at least mono-substituted mono- orpolycyclic ring system and/or may be bonded via an unsubstituted or atleast mono-substituted C₁₋₅ alkylene group, C₂₋₅ alkenylene group orC₂₋₅ alkinylene group; a —P(═O)(OR¹⁶)₂ moiety; a —C(═O)—OR¹⁷ moiety; a—C(═O)—NH—R¹⁸ moiety or a —C(═O)—R¹⁹ moiety; R⁷ and R⁸, independently ofone another, in each case represent a hydrogen atom; an unsubstituted orat least mono-substituted C₁₋₁₆ alkyl radical, C₂₋₁₆ alkenyl radical orC₂₋₁₆ alkinyl radical; an unsubstituted or at least mono-substitutedC₃₋₁₆ cycloalkyl radical or C₄₋₁₆ cycloalkenyl radical, which in eachcase may be condensed with an unsubstituted or at least mono-substitutedmono- or polycyclic ring system and/or may be bridged by at least oneunsubstituted or at least mono-substituted C₁₋₅ alkylene group and/ormay be bonded via an unsubstituted or at least mono-substituted C₁₋₅alkylene group, C₂₋₅ alkenylene group or C₂₋₅ alkinylene group; anunsubstituted or at least mono-substituted C₄₋₁₆ heterocycloalkylradical or C₅₋₁₆ heterocycloalkenyl radical, which in each case may becondensed with an unsubstituted or at least mono-substituted mono- orpolycyclic ring system and/or may be bridged by at least oneunsubstituted or at least mono-substituted C₁₋₅ alkylene group and/ormay be bonded via an unsubstituted or at least mono-substituted C₁₋₅alkylene group, C₂₋₅ alkenylene group or C₂₋₅ alkinylene group; anunsubstituted or at least mono-substituted C₃₋₁₆ cycloalkyl radical,C₄₋₁₆ cycloalkenyl radical, C₄₋₁₆ heterocycloalkyl radical or C₅₋₁₆heterocycloalkenyl radical which together with an unsubstituted or atleast mono-substituted C₃₋₁₆ cycloalkyl radical, C₄₋₁₆ cycloalkenylradical, C₄₋₁₆ heterocycloalkyl radical or C₅₋₁₆ heterocycloalkenylradical forms an unsubstituted or at least mono-substituted spirocyclicresidue via a common ring atom; an unsubstituted or at leastmono-substituted 6- or 10-membered aryl radical, which may be condensedwith an unsubstituted or at least mono-substituted mono- or polycyclicring system and/or may be bonded via an unsubstituted or at leastmono-substituted C₁₋₅ alkylene group, C₂₋₅ alkenylene group or C₂₋₅alkinylene group; an unsubstituted or at least mono-substituted 5- to14-membered heteroaryl radical, which may be condensed with anunsubstituted or at least mono-substituted mono- or polycyclic ringsystem and/or may be bonded via an unsubstituted or at leastmonosubstituted C₁₋₅ alkylene group, C₂₋₅ alkenylene group or C₂₋₅alkinylene group; a —P(═O)(OR¹⁶)₂ moiety; a —C(═O)—OR¹⁷ moiety; a—C(═O)—NH—R¹⁸ moiety; a —C(═O)—R¹⁹ moiety; a —S(═O)₂—R²⁰ moiety; or a—NR²¹R²² moiety; R⁹ represents a hydrogen atom or an unsubstituted or atleast mono-substituted C₁₋₁₆ alkyl radical, C₂₋₁₆ alkenyl radical orC₂₋₁₆ alkinyl radical; R¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²⁰,independently of one another, in each case represent an unsubstituted orat least mono-substituted C₁₋₁₆ alkyl radical, C₂₋₁₆ alkenyl radical orC₂₋₁₆ alkinyl radical; an unsubstituted or at least mono-substitutedC₃₋₁₆ cycloalkyl radical or C₄₋₁₆ cycloalkenyl radical, which in eachcase may be condensed with an unsubstituted or at least mono-substitutedmono- or polycyclic ring system and/or may be bridged by at least oneunsubstituted or at least mono-substituted C₁₋₅ alkylene group and/ormay be bonded via an unsubstituted or at least mono-substituted C₁₋₅alkylene group, C₂₋₅ alkenylene group or C₂₋₅ alkinylene group; anunsubstituted or at least mono-substituted C₄₋₁₆ heterocycloalkylradical or C₅₋₁₆ heterocycloalkenyl radical, which in each case may becondensed with an unsubstituted or at least mono-substituted mono- orpolycyclic ring system and/or may be bridged by at least oneunsubstituted or at least mono-substituted C₁₋₅ alkylene group and/ormay be bonded via an unsubstituted or at least mono-substituted C₁₋₅alkylene group, C₂₋₅ alkenylene group or C₂₋₅ alkinylene group; anunsubstituted or at least mono-substituted 6- or 10-membered arylradical, which may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bondedvia an unsubstituted or at least mono-substituted C₁₋₅ alkylene group,C₂₋₅ alkenylene group or C₂₋₅ alkinylene group; or an unsubstituted orat least mono-substituted 5- to 14-membered heteroaryl radical, whichmay be condensed with an unsubstituted or at least mono-substitutedmono- or polycyclic ring system and/or may be bonded via anunsubstituted or at least mono-substituted C₁₋₅ alkylene group, C₂₋₅alkenylene group or C₂₋₅ alkinylene group; R¹⁶, R¹⁷, R¹⁸ and R¹⁹,independently of one another, in each case represent an unsubstituted orat least mono-substituted C₁₋₁₆ alkyl radical, C₂₋₁₆ alkenyl radical orC₂₋₁₆ alkinyl radical; or an unsubstituted or at least mono-substituted6- or 10-membered aryl radical, which may be condensed with anunsubstituted or at least mono-substituted mono- or polycyclic ringsystem and/or may be bonded via an unsubstituted or at leastmono-substituted C₁₋₅ alkylene group, C₂₋₅ alkenylene group or C₂₋₅alkinylene group; or an unsubstituted or at least mono-substituted 5- to14-membered heteroaryl radical, which may be condensed with anunsubstituted or at least mono-substituted mono- or polycyclic ringsystem and/or may be bonded via an unsubstituted or at leastmono-substituted C₁₋₅ alkylene group, C₂₋₅ alkenylene group or C₂₋₅alkinylene group; and R²¹ and R²², independently of one another, in eachcase represent a hydrogen atom; an unsubstituted or at leastmono-substituted C₁₋₁₆ alkyl radical, C₂₋₁₆ alkenyl radical or C₂₋₁₆alkinyl radical; an unsubstituted or at least mono-substituted C₃₋₁₆cycloalkyl radical or C₄₋₁₆ cycloalkenyl radical, which in each case maybe condensed with an unsubstituted or at least mono-substituted mono- orpolycyclic ring system and/or may be bonded via an unsubstituted or atleast mono-substituted C₁₋₅ alkylene group, C₂₋₅ alkenylene group orC₂₋₅ alkinylene group; an unsubstituted or at least mono-substitutedC₄₋₁₆ heterocycloalkyl radical or C₅₋₁₆ heterocycloalkenyl radical,which in each case may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bondedvia an unsubstituted or at least mono-substituted C₁₋₅ alkylene group,C₂₋₅ alkenylene group or C₂₋₅ alkinylene group; an unsubstituted or atleast mono-substituted C₃₋₁₆ cycloalkyl radical, C₄₋₁₆ cycloalkenylradical, C₄₋₁₆ heterocycloalkyl radical or C₅₋₁₆ heterocycloalkenylradical which together with an unsubstituted or at leastmono-substituted C₃₋₁₆ cycloalkyl radical, C₄₋₁₆ cycloalkenyl radical,C₄₋₁₆ heterocycloalkyl radical or C₅₋₁₆ heterocycloalkenyl radical formsan unsubstituted or at least mono-substituted spirocyclic residue via acommon ring atom; an unsubstituted or at least mono-substituted 6- or10-membered aryl radical, which may be condensed with an unsubstitutedor at least mono-substituted mono- or polycyclic ring system and/or maybe bonded via an unsubstituted or at least mono-substituted C₁₋₅alkylene group, C₂₋₅ alkenylene group or C₂₋₅ alkinylene group; or anunsubstituted or at least mono-substituted 5- to 14-membered heteroarylradical, which may be condensed with an unsubstituted or at leastmono-substituted mono- or polycyclic ring system and/or may be bondedvia an unsubstituted or at least mono-substituted C₁₋₅ alkylene group,C₂₋₅ alkenylene group or C₂₋₅ alkinylene group; whereby the rings of theaforementioned ring system are in each case independently of one another5- 6- or 7-membered and may in each case independently of one anotheroptionally contain 1, 2 or 3 heteroatom(s) independently selected fromthe group consisting of nitrogen, oxygen and sulfur; the aforementionedheteroaryl radicals in each case optionally contain 1, 2, 3 or 4heteroatom(s) independently selected from the group consisting ofnitrogen, oxygen and sulfur as ring member(s); the aforementionedheterocycloalkyl radicals and heterocycloalkenyl radicals in each caseoptionally contain 1, 2, 3 or 4 heteroatom(s) independently selectedfrom the group consisting of nitrogen, oxygen and sulfur as ringmember(s); optionally in form of one of its stereoisomers, preferablyenantiomers or diastereomers, a racemate or in form of a mixture of atleast two of its stereoisomers, preferably enantiomers and/ordiastereomers, in any mixing ratio, or a corresponding N-oxide thereof,or a physiologically acceptable salt thereof, or a corresponding solvatethereof.
 3. A compound according to claim 1, characterized in that R¹and R², independently of one another, in each case represent a radicalselected from the group consisting of phenyl, naphthyl, pyridinyl, furyl(furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl,thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl,thiadiazolyl, triazolyl, pyridazinyl, indolyl, isoindolyl, pyrimidinyl,pyrazinyl, quinolinyl, isoquinolinyl, benzo[b]furanyl,benzo[b]thiophenyl, benzo[2,1,3]thiadiazolyl, [1,2,3]-benzothiadiazolyl,[2,1,3]-benzoxadiazolyl, [1,2,3]-benzoxadiazolyl, benzoxazolyl,benzthiazolyl, benzisoxazolyl, benzisothiazolyl,imidazo[2,1-b]thiazolyl, 2H-chromenyl, pyranyl, indazolyl, quinazolinyl,[1,3]-benzodioxolyl, [1,4]-benzodioxanyl, [1,2,3,4]-tetrahydronaphthyl,(2,3)-dihydro-1H-cyclopenta[b]indolyl, [1,2,3,4]-tetrahydroquinolinyl,[1,2,3,4]-tetrahydroisoquinolinyl, [1,2,3,4]-tetrahydroquinazolinyl and[3,4]-dihydro-2H-benzo[1,4]oxazinyl, which in each case is optionallybonded to the pyrazoline compound of general formula I via the aromaticor heteroaromatic part of the aforementioned radicals and may optionallybe substituted with 1, 2, 3, 4 or 5 substituent(s) independentlyselected from the group consisting of —CF₃, —CH₂—Cl, methyl, ethyl,n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂CH₂—CH₃,—S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃,—SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅,—C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃,—S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, phenoxy and thiophenyl, wherebythe thiophenyl radical can be substituted with 1, 2 or 3 substituentsindependently selected from the group consisting of F, Cl, Br, methyl,ethyl and n-propyl; or a radical selected from the group consisting ofcyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl,cyclooctyl, cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl,cyclotridecyl, cyclotetradecyl, cyclopentenyl, cyclohexenyl,cycloheptenyl, cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl,thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl,azepanyl, diazepanyl, azocanyl, (2,5)-dihydrofuranyl,(2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl, (2,3)-dihydrofuranyl,(2,5)-dihydro-1H-pyrrolyl, (2,3)-dihydro-1H-pyrrolyl,tetrahydrothiopyranyl, tetrahydropyranyl, (3,4)-dihydro-2H-pyranyl,(3,4)-dihydro-2H-thiopyranyl, (1,2,3,6)-tetrahydropyridinyl,(1,2,3,4)-tetrahydropyridinyl, (1,2,5,6)-tetrahydropyridinyl,[1,3]-oxazinanyl, hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl,oxazolidinyl, (1,3)-dioxanyl, (1,4)-dioxanyl, (1,3)-dioxolanyl,indolinyl, isoindolinyl, decahydronaphthyl,(1,2,3,4)-tetrahydroquinolinyl, (1,2,3,4)-tetrahydroisoquinolinyl,octahydro-cyclopenta[c]pyrrolyl, (1,3,4,7,9a)-hexahydro2H-quinolizinyl,(1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,(6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,(2,3)-dihydro-1H-benzo[de]isoquinolinyl,(1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,bicyclo[3.1.1]heptyl and norbornenyl, which in each case is optionallybonded to the pyrazoline compound of general formula I via the(hetero)cycloaliphatic part of the aforementioned radicals and mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of oxo (═O), thioxo(═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,—S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F,Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,—S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—CH₂H₅, —N(CH₃)₂ and—N(C₂H₅)₂.
 4. A compound according to claim 1, characterized in that R³represents a radical selected from the group consisting of(2,3)-dihydro-1H-cyclopenta[b]indolyl, cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl, cyclotetradecyl,cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, pyrrolidinyl,piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl,azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, azepanyl, diazepanyl, azocanyl,(2,5)-dihydrofuranyl, (2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl,(2,3)-dihydrofuranyl, (2,5)-dihydro-1H-pyrrolyl,(2,3)-dihydro-1H-pyrrolyl, tetrahydrothiopyranyl, tetrahydropyranyl,(3,4)-dihydro-2H-pyranyl, (3,4)-dihydro-2H-thiopyranyl,(1,2,3,6)-tetrahydropyridinyl, (1,2,3,4)-tetrahydropyridinyl,(1,2,5,6)-tetrahydropyridinyl, [1,3]-oxazinanyl, hexahydropyrimidinyl,(5,6)-dihydro-4H-pyrimidinyl, oxazolidinyl, (1,3)-dioxanyl,(1,4)-dioxanyl, (1,3)-dioxolanyl, indolinyl, isoindolinyl,decahydronaphthyl, (1,2,3,4)-tetrahydroquinolinyl,(1,2,3,4)-tetrahydroisoquinolinyl, octahydro-cyclopenta[c]pyrrolyl,(1,3,4,7,9a)-hexahydro-2H-quinolizinyl,(1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,dodecahydrocarbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,(6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,(2,3)-dihydro-1H-benzo[de]isoquinolinyl,(1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,bicyclo[3.1.1]heptyl, norbornenyl, 8-aza-bicyclo[3.2.1]octyl and8-aza-spiro[4.5]decanyl, which may optionally be substituted with 1, 2,3, 4 or 5 substituent(s) independently selected from the groupconsisting of oxo (═O), thioxo (═S), —CF₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl,n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —O—CH₂—O—CH₃, —O—CH₂—CH₂—O—CH₃,—O—CH₂—O—C₂H₅, —C(OCH₃)(C₂H₅)₂, —C(OCH₃)(CH₃)₂, —S—CH₃, —S—C₂H₅,—S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br,I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃,—C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,—S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, S(═O)—C₂H₅,—S(═O)—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —O—-Benzyl,benzyl, cyclopentyl, cyclohexyl, pyrrolidinyl and piperidinyl; a —O—R⁶moiety; a —NR⁷R⁸ moiety or a —NR⁹—O—R¹⁰ moiety.
 5. A compound accordingto claim 1, characterized in that R⁴ represents F; Cl; Br; I; —CN; —NO₂;—NC; —OH; —NH₂; —SH; —C(═O)—H; —C(═O)—OH; —C(═O)—OR ¹⁷; a radicalselected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl,3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl,3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl and 4-octyl, which mayoptionally be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9substituent(s) independently selected from the group consisting of —OH,F, Cl, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,—N(C₂H₅)₂, —CN and —NO₂; a radical selected from the group consisting ofphenyl, naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl),pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyland isoindolyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,—(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may optionally be substitutedwith 1, 2, 3, 4 or 5 substituent(s) independently selected from thegroup consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃,—O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,—S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃,—S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH,—NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—CH₂H₅,—N(CH₃)₂ and —N(C₂H₅)₂; a radical selected from the group consisting ofcyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl,cyclooctyl, cyclononyl, cyclodecyl, cyclopentenyl, cyclohexenyl,cycloheptenyl, cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl,thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl,azepanyl and diazepanyl, which may optionally be substituted with 1, 2,3, 4 or 5 substituent(s) independently selected from the groupconsisting of oxo (═O), thioxo (═S), —CF₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl,n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃,—S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃,—SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, ——NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅,—C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃,—S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ , and —N(C₂H₅)₂; a —O—R¹¹ moiety; a —S—R¹²moiety, a —NH—R¹³ moiety or a —NR¹⁴R¹⁵ moiety.
 6. A compound accordingto claim 1, characterized in that R⁴ and R⁵ together with the bridgingcarbon atom form a radical selected from the group consisting ofcyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl,cyclooctyl, cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl,cyclotridecyl, cyclotetradecyl, cyclopentenyl, cyclohexenyl,cycloheptenyl, and cyclooctenyl, which may optionally be substitutedwith 1, 2, 3, 4 or 5 substituent(s) independently selected from thegroup consisting of oxo (═O), thioxo (═S), —CF₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃,—S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃,—SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅,—C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃,—S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂.
 7. A compound according toclaim 1, characterized in that R⁵ represents H; F; Cl; Br; I; —CN; —NO₂;—NC; —OH; —NH₂; —SH; —C(═O)—H; —C(═O)—OH; —C(═O)—OR¹⁷; a radicalselected from the group consisting of methyl, —CF₃, —CH₂F, —CF₂H, —C₂F₅,ethyl, —CH₂—CN, —CH₂—OH, n-propyl, isopropyl, —CH₂—CH₂—CN, —CH₂—CH₂—OH,n-butyl, —CH₂—CH₂—CH₂—CN, —CH₂—CH₂—CH₂—OH, isobutyl, sec-butyl,tert-butyl, n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyland 3-hexyl; a radical selected from the group consisting ofcyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl,cyclooctyl, cyclononyl, cyclodecyl, cyclopentenyl, cyclohexenyl,cycloheptenyl, cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl,thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl,azepanyl and diazepanyl, a radical selected from the group consisting ofphenyl, naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl) andpyrrolyl, which may be bonded via a —(CH₂)— group and/or may optionallybe substituted with 1, 2, 3, 4 or 5 substituent(s) independentlyselected from the group consisting of —CF₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl,n-hexyl, —O—CH₃, —O—C₂H₅, F, Cl and Br; a —O—R¹¹ moiety; a —S—R¹²moiety, a —NH—R¹³ moiety or a —NR¹⁴R¹⁵ moiety.
 8. A compound accordingto claim 1, characterized in that R⁶ represents a hydrogen atom; aradical selected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl,3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl,3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl, 4-octyl vinyl,n-propenyl, n-butenyl, n-pentenyl, n-hexenyl, ethinyl, propinyl,n-butinyl, n-pentinyl and n-hexinyl, which may optionally be substitutedwith 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituent(s) independently selectedfrom the group consisting of —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —CN, —NO, —NH—C(═O)—CH₃,—NH—C(═O)—C₂H₅, —NH—C(═O)—C(CH₃)₃, —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅,—NH—C(═O)—O—C(CH₃)₃, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C(CH₃)₃,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅ and —C(═O)—C(CH₃)₃; a radicalselected from the group consisting of cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,cyclodecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl,pyrrolidinyl, piperidinyl, piperazinyl, homopiperazinyl, morpholinyl,aziridinyl, azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, azepanyl,8-aza-bicyclo[3.2.1]octyl and diazepanyl, which may be bonded via a—(CH₂)—, —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of oxo (═O), thioxo(═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,—S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F,Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,—S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and—N(C₂H₅)₂; a radical selected from the group consisting of phenyl,naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl,oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyl andisoindolyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,—(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may optionally be substitutedwith 1, 2, 3, 4 or 5 substituent(s) independently selected from thegroup consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃,—O—C₂H₅, —O—CH₂—CH₂—CH₃—O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,—S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃,—S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH,—NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂, —N(C₂H₅)₂, —O—C(50 O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂,—O—C(═O)—CH₂—CH₂—CH₃, —CH₂—N(CH₃)₂, —(CH₂)—N(C₂H₅)₂, —CH₂—N(C₃H₇)₂,—CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅) and —(CH₂)-morpholinyl; a —P(═O)(OR¹⁶)₂moiety; a —C(═O)—OR1¹⁷ moiety; a —C(═O)—NH—R¹⁸ moiety or a —C(═O)—R¹⁹moiety.
 9. A compound according to claim 1 , characterized in that R⁷and R⁸, independently of another, in each case represent a hydrogenatom; a radical selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl,2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl,2-heptyl, 3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl, 4-octyl,2-(6-methyl)-heptyl, 2-(5-methyl)-heptyl, 2-(5-methyl)-hexyl,2-(4-methyl)-hexyl, 2-(7-methyl)-octyl; 2-(6-methyl)-octyl, vinyl,n-propenyl, n-butenyl, n-pentenyl, n-hexenyl, ethinyl, propinyl,n-butinyl, n-pentinyl and n-hexinyl, which may optionally be substitutedwith 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituent(s) independently selectedfrom the group consisting of —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,—N(C₂H₅)₂, —CN and —NO₂; a radical selectedfrom the group consisting of (1,2,3,4)-tetrahydronaphthyl,(2,3)-dihydro-1H-cyclopenta[b]indolyl, cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl, cyclotetradecyl,cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, pyrrolidinyl,piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl,azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, azepanyl, diazepanyl, azocanyl,(2,5)-dihydrofuranyl, (2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl,(2,3)-dihydrofuranyl, (2,5)-dihydro-1H-pyrrolyl,(2,3)-dihydro-1H-pyrrolyl, tetrahydrothiopyranyl, tetrahydropyranyl,(3,4)-dihydro-2H-pyranyl, (3,4)-dihydro-2H-thiopyranyl,(1,2,3,6)-tetrahydropyridinyl, (1,2,3,4)-tetrahydropyridinyl, (1,2,5,6)-tetrahydropyridinyl, [1,3]-oxazinanyl, hexahydropyrimidinyl,(5,6)-dihydro4H-pyrimidinyl, oxazolidinyl, (1,3)-dioxanyl,(1,4)-dioxanyl, (1,3)-dioxolanyl, indolinyl, isoindolinyl,decahydronaphthyl, (1,2,3,4)-tetrahydroquinolinyl,(1,2,3,4)-tetrahydroisoquinolinyl, octahydro-cyclopenta[c]pyrrolyl,(1,3,4,7,9a)-hexahydro-2H-quinolizinyl,(1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,(6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,(2,3)-dihydro-1H-benzo[de]isoquinolinyl,(1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,bicyclo[3.1.1]heptyl, norbornenyl, 8-aza-bicyclo[3.2. 1]octyl and8-aza-spiro[4.5]decanyl, which may be bonded via a —(CH₂)—,—(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of oxo (═O), thioxo(═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,—O—CH₂—O—CH₃, —O—CH₂—CH₂—O—CH₃, —O—CH₂—O—C₂H₅, —C(OCH₃)(C₂H₅)₂,—C(OCH₃)(CH₃)₂, —S—CH₃, —S—C₂H₅, —S—CH₂CH₂—CH₃, —S—CH(CH₃)₂,—S—CH2—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H,—SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃,—C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —CF₂H, —CFH₂,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH3)2, —N(C₂H₅)₂, —O-Benzyl, benzyl, cyclopentyl, cyclohexyl,pyrrolidinyl and piperidinyl; a radical selected from the groupconsisting of phenyl, naphthyl, pyridinyl, furyl (furanyl), thienyl(thiophenyl), pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl,imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl,pyridazinyl, indolyl and isoindolyli, which may be bonded via a —(CH₂)—,—(CH₂) —(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of —CF₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃,—S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃,—SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅,—C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃,—S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂; a —P(═O)(OR¹⁶)₂ moiety; a—C(═O)—OR¹⁷ moiety; a —C(═O)—NH—R¹⁸ moiety; a —C(═O)—R¹⁹ moiety; a—S(═O)₂—R20 moiety; or a —NR²¹R²² moiety.
 10. A compound according toclaim 1 , characterized in that R⁹ represents hydrogen or an alkylradical selected from the group consisting of methyl, ethyl andn-propyl.
 11. A compound according to claim 1 , characterized in thatR¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²⁰, independently of another, in eachcase represent a radical selected from the group consisting of methyl,ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl,n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl,n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl,4-octyl, 2-(6-methyl)-heptyl, 2-(5-methyl)-heptyl, 2-(5-methyl)-hexyl,2-(4-methyl)-hexyl, 2-(7-methyl)-octyl; 2-(6-methyl)-octyl, vinyl,n-propenyl, n-butenyl, n-pentenyl, n-hexenyl, ethinyl, propinyl,n-butinyl, n-pentinyl and n-hexinyl, which may optionally be substitutedwith 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituent(s) independently selectedfrom the group consisting of —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —CN and —NO₂; a radical selectedfrom the group consisting of cyclopropyl, cyclobutyl, cyclopentyl,cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, cyclodecyl,cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, pyrrolidinyl,piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl,azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, azepanyl,8-aza-bicyclo[3.2.1]octyl and diazepanyl, which may be bonded via a—(CH₂)—, —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)—or —CH═CH— group and/or mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of oxo (═O), thioxo(═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,—S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F,Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,—C(—O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(—O)₂—CH₃,—S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and—N(C₂H₅)₂; or a radical selected from the group consisting of phenyl,naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl,oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyl andisoindolyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,—(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or may optionally besubstituted with 1, 2, 3, 4 or 5 substituent(s) independently selectedfrom the group consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,—O—CH₃, —O—C₂H₅, —O—CH₂—CH2CH₃, —O—CH(CH₃)₂, —O—CH2—CH2—CH₂—CH₃,—O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,—S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H,—SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃,—CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂ and —N(C₂H₅)₂.
 12. A compound according to claim 1 ,characterized in that R¹⁶, R¹⁷, R¹⁸ and R¹⁹, independently of oneanother, in each case represent a radical selected from the groupconsisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl,n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl,n-octyl, 2-octyl, 3-octyl, 4-octyl, vinyl, n-propenyl, n-butenyl,n-pentenyl, n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl andn-hexinyl, which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7,8 or 9 substituent(s) independently selected from the group consistingof NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH—C(═O)—CH₃,—NH—C(═O)—C₂H₅, —NH—C(═O)—C(CH₃)₃, —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅,—NH—C(═O)—O—C(CH₃)₃, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C(CH₃)₃,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —OH, —C(═O)—OH, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅ and—C(═O)—C(CH₃)₃; or a radical selected from the group consisting ofphenyl, naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl),pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyland isoindolyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,—(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or may optionally besubstituted with 1, 2, 3, 4 or 5 substituent(s) independently selectedfrom the group consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,—O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃,—O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,—S—CH₂—CH₂—CH,CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H,—SCFH₂, —OH, —SH, —NO_(2,) —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅,—C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃,—S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅,—O—C(═O)—CH(CH₃)₂, —O—C(═O)—CH₂—CH₂—CH₃, —CH₂—N(CH₃)₂, —(CH₂)—N(C₂H₅)₂,—CH₂—N(C₃H₇)₂, —CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅) and —(CH₂)-morpholinyl.13. A compound according to claim 1 , characterized in that R²¹ andR^(22,) independently of another, in each case represent hydrogen; aradical selected from the group consisting of methyl, ethyl, n-propyl, 5isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl,3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl,3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl, 4-octyl,2-(6-methyl)-heptyl, 2-(5-methyl)-heptyl, 2(5-methyl)-hexyl,2-(4-methyl)-hexyl, 2-(7-methyl)-octyl; 2-(6-methyl)-octyl, vinyl,n-propenyl, n-butenyl, n-pentenyl, n-hexenyl, ethinyl, propinyl,n-butinyl, n-pentinyl and n-hexinyl, which may optionally be substitutedwith 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituent(s) independently selectedfrom the group consisting of —OH, F. Cl, Br, I, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —CN and —NO₂; a radical selectedfrom the group consisting of (2,3)-dihydro-1H-cyclopenta[b]indolyl,cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl,cyclooctyl, cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl,cyclotridecyl, cyclotetradecyl, cyclopentenyl, cyclohexenyl,cycloheptenyl, cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl,thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl,azepanyl, diazepanyl, azocanyl, (2,5)-dihydrofuranyl,(2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl, (2,3)-dihydrofuranyl,(2,5)-dihydro-1H-pyrrolyl, (2,3)-dihydro-1H-pyrrolyl,tetrahydrothiopyranyl, tetrahydropyranyl, (3,4)-dihydro-2H-pyranyl,(3,4)-dihydro-2H-thiopyranyl, (1,2,3,6)-tetrahydropyridinyl,(1,2,3,4)-tetrahydropyridinyl, (1,2,5,6)-tetrahydropyridinyl,[1,3]-oxazinanyl, hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl,oxazolidinyl, (1,3)-dioxanyl, (1,4)-dioxanyl, (1,3)-dioxolanyl,indolinyl, isoindolinyl, decahydronaphthyl,(1,2,3,4)-tetrahydroquinolinyl, (1,2,3,4)-tetrahydroisoquinolinyl,octahydro-cyclopenta[c]pyrrolyl, (1,3,4,7,9a)-hexahydro-2H-quinolizinyl,(1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,(6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,(2,3)-dihydro-1H-benzo[de]isoquinolinyl,(1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,bicyclo[3.1.1]heptyl, norbornenyl, 8-aza-bicyclo[3.2.1]octyl and8-aza-spiro[4.5]decanyl, which may be bonded via a —(CH₂)—,—(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of oxo (═O), thioxo(═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₃, —O—C(CH₃)₃, —O—CH₂—O—CH₃,—O—CH₂—CH₂—O—CH₃, —O—CH₂—O—C₂H₅, —C(OCH₃)(C₂H₅)₂, —C(OCH₃)(CH₃)₂,—S—CH₃, —S—C₂H₅, —S—CH₂—CH₂CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃,—S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH,—NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —C(═O)—OH,—C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,—S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,—N(C₂H₅)₂, cyclopentyl, cyclohexyl, pyrrolidinyl and piperidinyl; or aradical selected from the group consisting of phenyl, naphthyl,pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl,isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl,thiadiazolyl, triazolyl, pyridazinyl, indolyl and isoindolyl, which maybe bonded via a —(CH₂)—, —(CH₂) —(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH—group and/or may optionally be substituted with 1, 2, 3, 4 or 5substituent(s) independently selected from the group consisting of —CF₃,methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl,tert-butyl, n-pentyl, 2-pentyl,.n-hexyl, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,—S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F,Cl, Br, I, —CN, —OCF₃—SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO_(2,) —CHO,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,—S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and—N(C₂H₅)₂.
 14. A compound according to claim 1 , characterized in that Xis S or O; R¹ and R², independently of one another, in each caserepresent a radical selected from the group consisting of phenyl,naphthyl, pyridinyl, furyl (furanyl); thienyl (thiophenyl), pyrrolyl,oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl,oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyl, isoindolyl,pyrimidinyl, pyrazinyl, quinolinyl, isoquinolinyl, benzo[b]furanyl,benzo[b]thiophenyl, benzo[2,1,3]thiadiazolyl, [1,2,3]-benzothiadiazolyl,[2,1,3]-benzoxadiazolyl, [1,2,3]-benzoxadiazolyl, benzoxazolyl,benzthiazolyl, benzisoxazolyl, benzisothiazolyliimidazo[2,1-b]thiazolyl, 2H-chromenyl, pyranyl, indazolyl, quinazolinyl,[1,31-benzodioxolyl, [1,4]benzodioxanyl, [1,2,3,4]-tetrahydronaphthyl,(2,3)-dihydro-lH-cyclopenta[b]indolyl, (1 ,2,3,4]-tetrahydroquinolinyl,[1 ,2,3,4]-tetrahydroisoquinolinyl, [1,2,3,4]-tetrahydroquinazolinyl and[3,4] dihydro-2H-benzo[1,4]oxazinyl, which in each case is optionallybonded to the pyrazoline compound of general formula I via the aromaticor heteroaromatic part of the aforementioned radicals and may optionallybe substituted with 1, 2, 3, 4 or 5 substituent(s) independentlyselected from the group consisting of —CF₃, —CH₂—Cl, methyl, ethyl,n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃,S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃,—SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(O) C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅,—C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH3,—S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, phenoxy and thiophenyl, wherebythe thiophenyl radical can be substituted with 1, 2 or 3 substituentsindependently selected from the group consisting of F, Cl, Br, methyl,ethyl and n-propyl; or a radical selected from the group consisting ofcyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl,cyclooctyl, cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl,cyclotridecyl, cyclotetradecyl, cyclopentenyl, cyclohexenyl,cycloheptenyl, cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl,thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl,azepanyl, diazepanyl, azocanyl, (2,5)-dihydrofuranyl,(2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl, (2,3)-dihydrofuranyl,(2,5)-dihydro-1H-pyrrolyl, (2,3)-dihydro-1H-pyrrolyl,tetrahydrothiopyranyl, tetrahydropyranyl, (3,4)-dihydro-2H-pyranyl,(3,4)-dihydro-2H-thiopyranyl, (1,2,3,6)-tetrahydropyridinyl,(1,2,3,4)-tetrahydropyridinyl, (1,2,5,6)-tetrahydropyridinyl,[1,3]-oxazinanyl, hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl,oxazolidinyl, (1,3)-dioxanyl, (1,4)-dioxanyl, (1,3)-dioxolanyl,indolinyl, isoindolinyl, decahydronaphthyl,(1,2,3,4)-tetrahydroquinolinyl, (1,2,3,4)-tetrahydroisoquinolinyl,octahydro-cyclopenta[c]pyrrolyli,(1,3,4,7,9a)-hexahydro-2H-quinolizinyl,(1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,dodecahydro-carbazolyli, 9H-carbazolyl, decahydroisoquinolinyl,(6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,(2,3)-dihydro-1H-benzo[de]isoquinolinyl,(1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,bicyclo[3.1.1]heptyl and norbornenyl, which in each case is optionallybonded to the pyrazoline compound of general formula I via the(hetero)cycloaliphatic part of the aforementioned radicals and mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of oxo (═O), thioxo(═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,—O—CH₂CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,—S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F,Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO_(2,) —CHO,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,—S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and—N(C₂H₅)₂; R³ represents a radical selected from the group consisting of(2,3)-dihydro-1H-cyclopenta[b]indolyl, cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl, cyclotetradecyl,cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, pyrrolidinyl,piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl,azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, azepanyl, diazepanyl, azocanyl,(2,5)-dihydrofuranyl, (2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl,(2,3)-dihydrofuranyl, (2,5)-dihydro-1H-pyrrolyl,(2,3)-dihydro-1H-pyrrolyl, tetrahydrothiopyranyl, tetrahydropyranyl,(3,4)-dihydro-2W-pyranyl, (3,4)-dihydro-2H-thiopyranyl,(1,2,3,6)-tetrahydropyridinyl, (1,2,3,4)-tetrahydropyridinyl,(1,2,5,6)-tetrahydropyridinyl, [1,3]-oxazinanyl, hexahydropyrimidinyl,(5,6)-dihydro-4H-pyrimidinyl, oxazolidinyl, (1,3)-dioxanyl,(1,4)-dioxanyl, (1,3)-dioxolanyl, indolinyl, isoindolinyl,decahydronaphthyl, (1 ,2,3,4)-tetrahydroquinolinyl,(1,2,3,4)-tetrahydroisoquinolinyl, octahydro-cyclopenta[c]pyrrolyl,(1,3,4,7,9a)-hexahydro-2H-quinolizinyl,(1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,(6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,(2,3)-dihydro-1H-benzo[de]isoquinolinyl,(1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,bicyclo[3.1.1]heptyl, norbornenyl, 8-aza-bicyclo[3.2.1]octyl and8-aza-spiro[4.5]decanyl, which may optionally be substituted with 1, 2,3, 4 or 5 substituent(s) independently selected from the groupconsisting of oxo (═O), thioxo (═S), —CF₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl,n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —O—CH₂—O—CH₃, —O—CH₂—CH₂—O—CH₃,—O—CH₂—O—C₂H₅, —C(OCH₃)(C₂H₅)₂, —C(OCH₃)(CH₃)₂, —S—CH₃, —S—C₂H₅,—S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br,I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃,—C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,—S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O—)₂—CH₃, —S(═O—)₂—C₂H₅,—S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —O-Benzyl,benzyl, cyclopentyl, cyclohexyl, pyrrolidinyl and piperidinyl; a —O—R⁶moiety; a —NR⁷R⁸ moiety or a —NR⁹—O—R¹⁰ moiety; R⁴ represents F; Cl; Br;I; —CN; —NO₂; —NC; —OH; —NH₂; —SH; —C(═O)—H; —C(═O)—OH; —C(═O)—OR⁷; aradical selected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl,3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl,3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl and 4-octyl, which mayoptionally be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9substituent(s) independently selected from the group consisting of —OH,F, Cl, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,—N(C₂H₅)₂, —CN and —NO₂; a radical selected from the group consisting ofphenyl, naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl),pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyland isoindolyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,—(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may optionally be substitutedwith 1, 2, 3, 4 or 5 substituent(s) independently selected from thegroup consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃,—O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,—S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃,—S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH,—NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂ and —N(C₂H₅)₂; a radical selected from the group consisting ofcyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl,cyclooctyl, cyclononyl, cyclodecyl, cyclopentenyl, cyclohexenyl,cycloheptenyl, cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl,thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl,azepanyl and diazepanyl, which may optionally be substituted with 1, 2,3, 4 or 5 substituent(s) independently selected from the groupconsisting of oxo (═O), thioxo (═S), —CF₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl,n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃,—S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃,—SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH_(3,)—C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,—S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅,—S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂; a —O—R¹¹moiety; a —S—R¹² moiety, a —NH—R¹³ moiety or a —NR¹⁴R¹⁵ moiety; R⁵represents H, F; Cl; Br; I; —CN; —NO₂; —NC; —OH; —NH₂; —SH; —C(═O)—H;—C(═O)—OH; —C(═O)—OR¹⁷; a radical selected from the group consisting ofmethyl, —CF₃, —CH₂F, —CF₂H, —C₂F₅, ethyl, —CH₂—CN, —CH₂—OH, n-propyl,isopropyl, —CH₂—CH₂—CN, —CH₂—CH₂—OH, n-butyl, —CH₂—CH₂—CH₂—CN,—CH₂—CH₂—CH₂—OH, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl,3-pentyl, neo-pentyl, n-hexyl, 2-hexyl and 3-hexyl; a radical selectedfrom the group consisting of cyclopropyl, cyclobutyl, cyclopentyl,cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, cyclodecyl,cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, pyrrolidinyl,piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl,azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, azepanyl and diazepanyl; aradical selected from the group consisting of phenyl, naphthyl,pyridinyl, furyl (furanyl), thienyl (thiophenyl) and pyrrolyl, which maybe bonded via a —(CH₂)-group and/or may optionally be substituted with1, 2, 3, 4 or 5 substituent(s) independently selected from the groupconsisting of —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃,—O—C₂H₅, F, Cl and Br; a —O—R¹¹ moiety; a —S—R¹² moiety, a —NH—R¹³moiety or a —NR¹⁴R¹⁵ moiety; R⁴ and R⁵ together with the bridging carbonatom form a radical selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl,cyclotetradecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, andcyclooctenyl, which may optionally be substituted with 1, 2, 3, 4 or 5substituent(s) independently selected from the group consisting of oxo(═O), thioxo (═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃,—O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,—S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃,—S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH,—NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂ and —N(C₂H₅)₂; R⁶ represents a hydrogen atom; a radicalselected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl,3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl,3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl, 4-octyl vinyl,n-propenyl, n-butenyl, n-pentenyl, n-hexenyl, ethinyl, propinyl,n-butinyl, n-pentinyl and n-hexinyl, which may optionally be substitutedwith 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituent(s) independently selectedfrom the group consisting of —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —CN, —NO, —NH—C(═O)—CH₃,—NH—C(═O)—C₂H₅, —NH—C(═O)—C(CH₃)₃, —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅,—NH—C(═O)—O—C(CH₃)₃, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C(CH₃)₃,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅ and —C(═O)—C(CH₃)₃; a radicalselected from the group consisting of cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,cyclodecyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl,pyrrolidinyl, piperidinyl, piperazinyl, homopiperazinyl, morpholinyl,aziridinyl, azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, azepanyl,8-aza-bicyclo[3.2.1]octyl and diazepanyl, which may be bonded via a—(CH₂)—, —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of oxo (═O), thioxo(═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,—S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F,Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,—S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and—N(C₂H₅)₂; a radical selected from the group consisting of phenyl,naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl,oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyl andisoindolyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,—(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may optionally be substitutedwith 1, 2, 3, 4 or 5 substituent(s) independently selected from thegroup consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃,—O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,—S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃,—S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SOF₃, —SCF₂H, —SCFH₂, —OH, —SH,—NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O—)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂, —N(C₂H₅)₂, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂,—O—C(═O)—CH₂—CH₂—CH₃, —CH₂—N(CH₃)₂, —(CH₂)—N(C₂H₅)₂ , —CH₂—N(C₃H₇)₂,—CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅) and —(CH₂)-morpholinyl; a —P(═O)(OR¹⁶)₂moiety; a —C(═O)—OR¹⁷ moiety; a —C(═O)—NH—R¹⁸ moiety or a —C(═O)—R¹⁹moiety; R⁷ and R⁸, independently of another, in each case represent ahydrogen atom; a radical selected from the group consisting of methyl,ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl,n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl,n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl,4-octyl, 2-(6-methyl)-heptyl, 2-(5-methyl)-heptyl, 2-(5-methyl)-hexyl,2-(4-methyl)-hexyl, 2-(7-methyl)-octyl; 2-(6-methyl)-octyl, vinyl,n-propenyl, n-butenyl, n-pentenyl, n-hexenyl, ethinyl, propinyl,n-butinyl, n-pentinyl and n-hexinyl, which may optionally be substitutedwith 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituent(s) independently selectedfrom the group consisting of —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —CN and —NO₂; a radical selectedfrom the group consisting of (1,2,3,4)-tetrahydronaphthyl,(2,3)-dihydro-1H-cyclopenta[b]indolyl, cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl, cyclotetradecyl,cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, pyrrolidinyl,piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl,azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, azepanyl, diazepanyl, azocanyl,(2,5)-dihydrofuranyl, (2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl,(2,3)-dihydrofuranyl, (2,5)-dihydro-1H-pyrrolyl,(2,3)-dihydro-1H-pyrrolyl, tetrahydrothiopyranyl, tetrahydropyranyl,(3,4)-dihydro-2H-pyranyl, (3,4)-dihydro-2H-thiopyranyl,(1,2,3,6)-tetrahydropyridinyl, (1,2,3,4)-tetrahydropyridinyl,(1,2,5,6)-tetrahydropyridinyl, [1,3]-oxazinanyl, hexahydropyrimidinyl,(5,6)-dihydro-4H-pyrimidinyl, oxazolidinyl, (1,3)-dioxanyl,(1,4)-dioxanyl, (1,3)-dioxolanyl, indolinyl, isoindolinyl,decahydronaphthyl, (1,2,3,4)-tetrahydroquinolinyl,(1,2,3,4)-tetrahydroisoquinolinyl, octahydro-cyclopenta[c]pyrrolyl,(1,3,4,7,9a)-hexahydro-2H-quinolizinyl,(1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,(6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,(2,3)-dihydro-1H-benzo[de]isoquinolinyl,(1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,bicyclo[3.1.1]heptyl, norbornenyl, 8-aza-bicyclo[3.2.1]octyl and8-aza-spiro[4.5]decanyl, which may be bonded via a —(CH₂)—,—(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may optionallybe substituted with 1, 2, 3, 4 or 5 (substituent(s) independentlyselected from the group consisting of oxo (═O), thioxo (═S), —CF₃,methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl,tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,—O—CH₂—O—CH₃, —O—CH₂—CH₂—O—CH₃, —O—CH₂—O—C₂H₅, —C(OCH₃)(C₂H₅)₂,—C(OCH₃)(CH₃)₂, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,—S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H,—SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃,—C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —CF₂H, —CFH₂,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂, —N(C₂H₅)₂, —O-Benzyl, benzyl, cyclopentyl, cyclohexyl,pyrrolidinyl and piperidinyl; a radical selected from the groupconsisting of phenyl, naphthyl, pyridinyl, furyl (furanyl), thienyl(thiophenyl), pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl,imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl,pyridazinyl, indolyl and isoindolyl, which may be bonded via a —(CH₂)—,—(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may optionallybe substituted with 1, 2, 3, 4 or 5 substituent(s) independentlyselected from the group consisting of —CF₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl,n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃,—S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃,—SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅,—C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃,—S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and —N(C₂H₅)₂; a —P(═O)(OR¹⁶)₂ moiety; a—C(═O)—OR¹⁷ moiety; a —C(═O)—NH—R¹⁸ moiety; a —C(═O)—R¹⁹ moiety; a—S(═O)₂—R²⁰ moiety; or a —NR²¹R²² moiety; R⁹ represents hydrogen or analkyl radical selected from the group consisting of methyl, ethyl andn-propyl. R¹⁰, R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²⁰, independently ofanother, in each case represent a radical selected from the groupconsisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl,n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl,n-octyl, 2-octyl, 3-octyl, 4-octyl, 2-(6-methyl)-heptyl,2-(5-methyl)-heptyl, 2-(5-methyl)-hexyl, 2-(4-methyl)-hexyl,2-(7-methyl)-octyl; 2-(6-methyl)-octyl, vinyl, n-propenyl, n-butenyl,n-pentenyl, n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl andn-hexinyl, which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7,8 or 9 substituent(s) independently selected from the group consistingof —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂,—N(C₂H₅)₂, —CN and —NO₂; a radical selected from the group consisting ofcyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl,cyclooctyl, cyclononyl, cyclodecyl, cyclopentenyl, cyclohexenyl,cycloheptenyl, cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl,thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl,azepanyl, 8-aza-bicyclo[3.2.1]octyl and diazepanyl, which may be bondedvia a —(CH₂)—, —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═—CH-groupand/or may optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of oxo (═O), thioxo(═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —C—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,—S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F,Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,—C(═O—)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,—S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and—N(C₂H₅)₂; or a radical selected from the group consisting of phenyl,naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl,oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyl andisoindolyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,—(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may optionally be substitutedwith 1, 2, 3, 4 or 5 substituent(s) independently selected from thegroup consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃,—O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,—S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃,—S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH,—NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂ and —N(C₂H₅)₂; R¹⁶, R¹⁷, R¹⁸ and R¹⁹, independently of oneanother, in each case represent a radical selected from the groupconsisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl,n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl,n-octyl, 2-octyl, 3-octyl, 4-octyl, vinyl, n-propenyl, n-butenyl,n-pentenyl, n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl andn-hexinyl, which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7,8 or 9 substituent(s) independently selected from the group consistingof NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH—C(═O)—CH₃,—NH—C(═O)—C₂H₅, —NH—C(═O)—C(CH₃)₃, —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅,—NH—C(═O)—O—C(CH₃)₃, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C(CH₃)₃,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —OH, —C(═O)—OH, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅ and—C(═O)—C(CH₃)₃; or a radical selected from the group consisting ofphenyl, naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl),pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyland isoindolyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,—(CH₂)—(CH₂)—(CH₂)— or —CH═CH-group and/or may optionally be substitutedwith 1, 2, 3, 4 or 5 substituent(s) independently selected from thegroup consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃,—O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,—S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃,—S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH,—NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂, —N(C₂H₅)₂, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂,—O—C(═O)—CH₂—CH₂—CH₃, —CH₂—N(CH₃)₂, —(CH₂)—N(C₂H₅)₂, —CH₂—N(C₃H₇)₂,—CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅) and —(CH₂)-morpholinyl; and R²¹ andR^(22,) independently of another, in each case represent hydrogen; aradical selected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl,3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl,3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl, 4-octyl,2-(6-methyl)-heptyl, 2-(5-methyl)-heptyl, 2-(5-methyl)-hexyl,2-(4-methyl)-hexyl, 2-(7-methyl)-octyl; 2-(6-methyl)-octyl, vinyl,n-propenyl, n-butenyl, n-pentenyl, n-hexenyl, ethinyl, propinyl,n-butinyl, n-pentinyl and n-hexinyl, which may optionally be substitutedwith 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituent(s) independently selectedfrom the group consisting of —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —CN and —NO₂; a radical selectedfrom the group consisting of (2,3)-dihydro-1H-cyclopenta[b]indolyl,cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl,cyclooctyl, cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl,cyclotridecyl, cyclotetradecyl, cyclopentenyl, cyclohexenyl,cycloheptenyl, cyclooctenyl, pyrrolidinyl, piperidinyl, piperazinyl,homopiperazinyl, morpholinyl, aziridinyl, azetidinyl, imidazolidinyl,thiomorpholinyl, pyrazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl,azepanyl, diazepanyl, azocanyl, (2,5)-dihydrofuranyl,(2,5)-dihydrothiophenyl, (2,3)-dihydrofuranyl, (2,3)-dihydrofuranyl,(2,5)-dihydro-1H-pyrrolyl, (2,3)-dihydro-1H-pyrrolyl,tetrahydrothiopyranyl, tetrahydropyranyl, (3,4)-dihydro-2H-pyranyl,(3,4)-dihydro-2H-thiopyranyl, (1,2,3,6)-tetrahydropyridinyl,(1,2,3,4)-tetrahydropyridinyl, (1,2,5,6)-tetrahydropyridinyl,[1,3]-oxazinanyl, hexahydropyrimidinyl, (5,6)-dihydro-4H-pyrimidinyl,oxazolidinyl, (1,3)-dioxanyl, (1,4)-dioxanyl, (1,3)-dioxolanyl,indolinyl, isoindolinyl, decahydronaphthyl,(1,2,3,4)-tetrahydroquinolinyl, (1,2,3,4)-tetrahydroisoquinolinyl,octahydro-cyclopenta[c]pyrrolyl, (1,3,4,7,9a)-hexahydro-2H-quinolizinyl,(1,2,3,5,6,8a)-hexahydro-indolizinyl, decahydroquinolinyl,dodecahydro-carbazolyl, 9H-carbazolyl, decahydroisoquinolinyl,(6,7)-dihydro-4H-thieno[3,2-c]pyridinyl,(2,3)-dihydro-1H-benzo[de]isoquinolinyl,(1,2,3,4)-tetrahydroquinoxazlinyl, adamantyl, bicyclo[2.2.1]heptyl,bicyclo[3.1.1]heptyl, norbornenyl, 8-aza-bicyclo[3.2.1]octyl and8-aza-spiro[4.5]decanyl, which may be bonded via a —(CH₂)—,—(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of oxo (═O), thioxo(═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃,—O—CH₂—O—CH₃, —O—CH₂—CH₂—O—CH₃, —O—CH₂—O—C₂H₅, —C(OCH₃)(C₂H₅)₂,—C(OCH₃)(CH₃)₂, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,—S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H,—SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃,—C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —CF₂H, —CFH₂,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂, —N(C₂H₅)₂, cyclopentyl, cyclohexyl, pyrrolidinyl andpiperidinyl; or a radical selected from the group consisting of phenyl,naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl,oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyl andisoindolyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,—(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or may optionally besubstituted with 1, 2, 3, 4 or 5 substituent(s) independently selectedfrom the group consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,—O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃,—O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,—S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H,—SCFH₂ —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃,—CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O) NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O) C₂H₅ —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH2, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂ and —N(C₂H₅)₂; optionally in form of one of its stereoisomers,preferably enantiomers or diastereomers, a racemate or in form of amixture of at least two of its stereoisomers, preferably enantiomersand/or diastereomers, in any mixing ratio, or a corresponding N-oxidethereof, or a physiologically acceptable salt thereof, or acorresponding solvate thereof.
 15. A compound according to claim 1 ,characterized in that X is O or S; R¹ represents a radical selected fromthe group consisting of phenyl, naphthyl, pyridinyl, furyl (furanyl),thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl, thiazolyl,isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl,triazolyI, pyridazinyl, indolyl, isoindolyl, pyrimidinyl, pyrazinyl,quinolinyl, isoquinolinyl, benzo[b]furanyl, benzo[b]thiophenyl,benzo[2,1,3]thiadiazolyl, [1,2,3]-benzothiadiazolyl,[2,1,3]-benzoxadiazolyl, [1,2,3]-benzoxadiazolyl, benzoxazolyl,benzthiazolyl, benzisoxazolyl, benzisothiazolyl andimidazo[2,1-b]thiazolyl, which may optionally be substituted with 1, 2,3, 4 or 5 substituent(s) independently selected from the groupconsisting of —CF₃, —CH₂—Cl, methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,—NO₂, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, I, —CN, —OCF_(3,) —SCF₃, —SCF₂H,—SCFH₂, phenoxy and thiophenyl, whereby the thiophenyl radical can besubstituted with 1, 2 or 3 substituents independently selected from thegroup consisting of F, Cl, Br, methyl, ethyl and n-propyl; or a radicalselected from the group consisting of cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, pyrrolidinyl,piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl,azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, azepanyl and diazepanyl, whichmay optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of —CF₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,2-pentyl, n-hexyl, F, Cl, Br, I, —CN, —OCF_(3,) —SCF₃, —SCF₂H and—SCFH₂; R² represents a radical selected from the group consisting ofphenyl, naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl),pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyl,isoindolyl, pyrinidinyl, pyrazinyl, quinolinyl, isoquinolinyl,benzo[b]furanyl, benzo[b]thiophenyl, benzo[2,1,3]thiadiazolyl,[1,2,3]-benzothiadiazolyl, [2,1,3]-benzoxadiazolyl,[1,2,3]-benzoxadiazolyl, benzoxazolyl, benzthiazolyl, benzisoxazolyl,benzisothiazolyl and imidazo[2,1-b]thiazolyl, which may optionally besubstituted with 1, 2, 3, 4 or 5 substituent(s) independently selectedfrom the group consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,—OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H and—SCFH₂; or a radical selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,cyclononyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl,pyrrolidinyl, piperidinyl, piperazinyl, homopiperazinyl, morpholinyl,aziridinyl, azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, azepanyl and diazepanyl, whichmay optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of —CF₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,2-pentyl, n-hexyl, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H and —SCFH₂;R³ represents a radical selected from the group consisting of

which is in each case bonded to the pyrazoline compound of generalformula I in any position of the cyclic part of the aforementionedradicals including the NH— groups, preferably said radicals are bondedto the pyrazoline compound of general formula I at the nitrogen atom ofthe cyclic part of the aforementioned radicals; a —O—R⁶ moiety, a —NR⁷R⁸moiety or a —NR⁹—O—R¹⁰ moiety; R⁴ represents F; Cl; Br; I; —CN; —NO₂;—NC; —OH; —NH₂; —SH; —C(═O)—H; —C(═O)—OH; —C(═O)—OR¹⁷; a radicalselected from the group consisting of methyl, —CF₃, —CH₂F, —CF₂H, —C₂F₅,ethyl, —CH₂—CN, —CH₂—OH, n-propyl, isopropyl, —CH₂—CH₂—CN, —CH₂—CH₂—OH,n-butyl, —CH₂—CH₂—CH₂—CN, —CH₂—CH₂—CH₂—OH, isobutyl, sec-butyl,tert-butyl, n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyland 3-hexyl; a radical selected from the group consisting of phenyl,naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl) and pyrrolyl,which may be bonded via a —(CH₂)— group and/or may optionally besubstituted with 1, 2, 3, 4 or 5 substituent(s) independently selectedfrom the group consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,—O—CH₃, —O—C₂H₅, F, Cl and Br; a —O—R¹¹ moiety; a —S—R¹² moiety, a—NH—R¹³ moiety or a —NR¹⁴R¹⁵ moiety; R⁵ represents H; F; Cl;Br;—C(═O)—OH; —C(═O)—OR¹⁷; or an alkyl radical selected from the groupconsisting of methyl, ethyl, n-propyl, isopropyl and n-butyl; or R⁴ andR⁵ together with the bridging carbon atom form a radical selected fromthe group consisting of cyclopropyl, cyclobutyl, cyclopentyl,cyclohexyl, cycloheptyl, cyclooctyl, cyclopentenyl, cyclohexenyl,cycloheptenyl and cyclooctenyl; R⁶ represents a hydrogen atom; a radicalselected from the group consisting of methyl, —CF₃, —CH₂F, —CF₂H,—CH₂—O—CH₃, —C₂F₅, —CH₂—CH₂—F, ethyl, —CH₂—CN, —CH₂—OH, n-propyl,isopropyl, —CH₂—CH₂—CN, —CH₂—CH₂—OH, —CH₂—CH₂—OCH₃, n-butyl,—CH₂—CH₂—CH₂—CN, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH2O—CH₃, isobutyl,sec-butyl, tert-butyl, n-pentyl, —CH₂—CH₂—CH₂—CH₂—O—CH₃, 2-pentyl,3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl and n-octyl; aradical selected from the group consisting of cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, cycloheptyl, pyrrolidinyl, piperidinyl,piperazinyl, homopiperazinyl, morpholinyl, imidazolidinyl, azepanyl,8-aza-bicyclo[3.2.1 ]octyl and diazepanyl, which may be bonded via a—(CH₂)—, —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of oxo (═O), thioxo(═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl,tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃ and —O—C(CH₃)₃; aradical selected from the group consisting of pyridinyl, furyl(furanyl), thienyl (thiophenyl), pyrrolyl, oxazolyl, isoxazolyl,thiazolyl, isothiazolyl and imidazolyl, which may be bonded via a—(CH₂)—, —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH=CH— group and/or mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, F, Cl, Br, I, —O—C(═O)—CH₃,—O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂, —O—C(═O)—CH₂—CH₂—CH₃, —CH₂—N(CH₃)₂,—(CH₂)—N(C₂H₅)₂, —CH₂—N(C₃H₇)₂, —CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅) and—(CH₂)-morpholinyl; a —P(═O)(OR¹⁶)₂ moiety; a —C(═O)—OR¹⁷ moiety; a—C(═O)—NH—R¹⁸ moiety or a —C(═O)—R¹⁹ moiety; R⁷ and R⁸, independently ofanother, in each case represent a hydrogen atom; a radical selected fromthe group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl,isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl,neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl,4-heptyl, n-octyl, 2-octyl, 3-octyl, 4-octyl, 2-(6-methyl)-heptyl,2-(5-methyl)-heptyl, 2-(5-methyl)-hexyl, 2-(4-methyl)-hexyl,2-(7-methyl)-octyl; 2-(6-methyl)-octyl, —CH₂—NH₂, —CH₂—N(CH₃)₂,—CH₂—CH—NH₂, —CH₂—CH₂—N(CH₃)₂, —CH₂—CH₂—N(C₂H₅)₂, —CH₂—CH₂—CH₂—NH₂,—CH₂—N(CH₃)₂ and —CH₂—CH₂—CH₂—N(C₂H₅)₂; a radical selected from thegroup consisting of morpholinyl, piperidinyl, pyrrolidinyl, cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,cyclononyl, cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl,cyclotetradecyl, [1,2,3,4]-tetrahydronaphthyl and bicyclo[2.2.1]heptyl,which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or—CH═CH— group and/or may optionally be substituted with 1, 2, 3, 4 or 5substituient(s) independently selected from the group consisting of —OH,—O—CH₃, —O—C₂H₅, —O-Benzyl, benzyl, methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl and n-hexyl;a radical selected from the group consisting of phenyl, naphthyl,pyridinyl, furyl (furanyl), thienyl (thiophenyl) and triazolyl, whichmay be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or—CH═CH— group and/or may optionally be substituted with 1, 2, 3, 4 or 5substituent(s) independently selected from the group consisting of —CF₃,methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl,tert-butyl, n-pentyl, 2-pentyl, n-hexyl, F, Cl and Br; a —S(═O)₂—R²⁰moiety; a —NR²¹ R²² moiety; a radical selected from the group consistingof

which is in each case bonded to the pyrazoline compound of generalformula I in any position of the cyclic part of the aforementionedradicals including the NH— groups, optionally via a —(CH₂)— or—(CH₂)—(CH₂)— group, preferably said radicals are bonded to thepyrazoline compound of general formula I at the nitrogen atom of thecyclic part of the aforementioned radicals; R⁹ represents hydrogen; R¹⁰,R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²⁰, independently of another, in each caserepresent a radical selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl,2-pentyl, 3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl,2-heptyl, 3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl, 4-octyl,2-(6-methyl)-heptyl, 2-(5-methyl)-heptyl, 2-(5-methyl)-hexyl,2-(4-methyl)-hexyl, 2-(7-methyl)-octyl; 2-(6-methyl)-octyl, vinyl,n-propenyl, n-butenyl, n-pentenyl, n-hexenyl, ethinyl, propinyl,n-butinyl, n-pentinyl and n-hexinyl, which may optionally be substitutedwith 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituent(s) independently selectedfrom the group consisting of —OH, F, Cl, Br, I, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —CN and —NO₂; a radical selectedfrom the group consisting of cyclopropyl, cyclobutyl, cyclopentyl,cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, cyclodecyl,cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, pyrrolidinyl,piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, aziridinyl,azetidinyl, imidazolidinyl, thiomorpholinyl, pyrazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, azepanyl,8-aza-bicyclo[3.2.1]octyl and diazepanyl, which may be bonded via a—(CH₂)—, —(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of oxo (═O), thioxo(═S), —CF₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, —O—CH₃, —O—C₂H₅,—O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, —O—C(CH₃)₃, —S—CH₃,—S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂, —S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F,Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H, —SCFH₂, —OH, —SH, —NO₂, —CHO,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CF₂H, —CFH₂, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇, —S(═O)₂—CH₃,—S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂ and—N(C₂H₅)₂; or a radical selected from the group consisting of phenyl,naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl), pyrrolyl,oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrazolyl,oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyl andisoindolyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,—(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or may optionally besubstituted with 1, 2, 3, 4 or 5 substituent(s) independently selectedfrom the group consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,—O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃,—O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,—S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H,—SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃,—CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH₃, —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂ and —N(C₂H₅)₂; R¹⁶, R¹⁷, R¹⁸ and R¹⁹, independently of oneanother, in each case represent a radical selected from the groupconsisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl,sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl, neo-pentyl,n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl,n-octyl, 2-octyl, 3-octyl, 4-octyl, vinyl, n-propenyl, n-butenyl,n-pentenyl, n-hexenyl, ethinyl, propinyl, n-butinyl, n-pentinyl andn-hexinyl, which may optionally be substituted with 1, 2, 3, 4, 5, 6, 7,8 or 9 substituent(s) independently selected from the group consistingof NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH—C(═O)—CH₃,—NH—C(═O)—C₂H₅, —NH—C(═O)—C(CH₃)₃, —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅,—NH—C(═O)—O—C(CH₃)₃, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C(CH₃)₃,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —OH, —C(═O)—OH, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅ and—C(═O)—C(CH₃)₃; or a radical selected from the group consisting ofphenyl, naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl),pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl,pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridazinyl, indolyland isoindolyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,—(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or may optionally besubstituted with 1, 2, 3, 4 or 5 substituent(s) independently selectedfrom the group consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl,—O—CH₃, —O—C₂H₅, —O—CH₂—CH₂—CH₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃,—O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH₂—CH₂—CH₃, —S—CH(CH₃)₂,—S—CH₂—CH₂—CH₂—CH₃, —S—C(CH₃)₃, F, Cl, Br, I, —CN, —OCF₃, —SCF₃, —SCF₂H,—SCFH₂, —OH, —SH, —NO₂, —CHO, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃,—CF₂H, —CFH₂, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—NH—C₃H₇,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —S(═O)—CH₃, —S(═O)—C₂H₅, —S(═O)—C₃H₇,—S(═O)₂—CH —S(═O)₂—C₂H₅, —S(═O)₂—C₃H₇, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂, —N(C₂H₅)₂, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂,—O—C(═O)—CH₂—CH₂—CH₃, —CH₂—N(CH₃)₂, —(CH₂)—N(C₂H₅)₂, —CH₂—N(C₃H₇)₂,—CH₂—N(C₄H₉)₂, —CH₂—N(CH₃)(C₂H₅) and —(CH₂)-morpholinyl; and R²¹ andR_(22,) independently of another, in each case represent hydrogen; aradical selected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl,3-pentyl, neo-pentyl, n-hexyl, 2-hexyl, 3-hexyl, n-heptyl, 2-heptyl,3-heptyl, 4-heptyl, n-octyl, 2-octyl, 3-octyl, 4-octyl,2-(6-methyl)-heptyl, 2-(5-methyl)-heptyl, 2-(5-methyl)-hexyl,2-(4-methyl)-hexyl, 2-(7-methyl)-octyl; 2-(6methyl)-octyl, —CH₂—NH₂,—CH—N(CH₃)₂, —CH₂—CH—NH₂, —CH₂—CH₂—N(CH₃)₂, —CH₂—CH₂—N(C₂H₅)₂,—CH₂—CH₂—CH₂—NH₂, —CH₂—CH₂—CH₂—N(CH₃)₂ and —CH₂—CH₂—CH₂—N(C₂H₅)₂; aradical selected from the group consisting of cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl,cyclodecyl, cycloundecyl, cyclododecyl, cyclotridecyl, cyclotetradecyland bicyclo[2.2.1]heptyl, which may be bonded via a —(CH₂)—,—(CH₂)—(CH₂)—, —(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or mayoptionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of —OH, methyl, ethyl,n-propyl, isopropyl, n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl,2-pentyl and n-hexyl; a radical selected from the group consisting ofphenyl, naphthyl, pyridinyl, furyl (furanyl), thienyl (thiophenyl) andtriazolyl, which may be bonded via a —(CH₂)—, —(CH₂)—(CH₂)—,—(CH₂)—(CH₂)—(CH₂)— or —CH═CH— group and/or may optionally besubstituted with 1, 2, 3, 4 or 5 substituent(s) independently selectedfrom the group consisting of —CF₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, isobutyl, 2-butyl, tert-butyl, n-pentyl, 2-pentyl, n-hexyl, F,Cl and Br; or a radical selected from the group consisting of

which is in each case bonded to the pyrazoline compound of generalformula I in any position of the cyclic part of the aforementionedradicals including the NH— groups, preferably said radicals are bondedto the pyrazoline compound of general formula I at the nitrogen atom ofthe cyclic part of the aforementioned radicals; optionally in form ofone of its stereoisomers, preferably enantiomers or diastereomers, aracemate or in form of a mixture of at least two of its stereoisomers,preferably enantiomers and/or diastereomers, in any mixing ratio, or acorresponding N-oxide thereof, or a physiologically acceptable saltthereof, or a corresponding solvate thereof.
 16. A compound according toclaim 1 , characterized in that x is O or S; R¹ represents a radicalselected from the group consisting of phenyl and thienyl (thiophenyl),which may optionally be substituted with 1, 2, 3, 4 or 5 substituent(s)independently selected from the group consisting of —OH, —O—CH₃,—O—C₂H₅, F, Cl, Br and I; R² represents a phenyl radical, which may besubstituted with 1, 2, 3, 4 or 5 substituent(s) independently selectedfrom the group consisting of —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br and I; R³represents a radical selected from the group consisting of

which is in each case bonded to the pyrazoline compound of generalformula I in any position of the cyclic part of the aforementionedradicals including the NH— groups, preferably said radicals are bondedto the pyrazoline compound of general formula I at the nitrogen atom ofthe cyclic part of the aforementioned radicals; a —OR⁶— moiety or a—NR⁷R⁸ moiety; R⁴ represents F; Cl; Br; I; —OH, —CN; —C(═O)—H;—C(═O)—OH; —C(═O)—OR¹⁷; a radical selected from the group consisting ofmethyl, —CF₃, —CH₂F, —CF₂H, —C₂F₅, ethyl, —CH₂—CN, —CH₂—OH, n-propyl,isopropyl, —CH₂—CH₂—CN, —CH₂—CH₂—OH, n-butyl, —CH₂—CH₂—CH₂—CN,—CH₂—CH₂—CH₂—OH, isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl,3-pentyl, neo-pentyl, n-hexyl, 2-hexyl and 3-hexyl; a benzyl radical ora —O—R¹¹ moiety; R⁵ represents H; F; Cl; Br;—C(═O)—OH; —C(═O)—OR¹⁷; or aradical selected from the group consisting of methyl, ethyl, n-propyl,iso-propyl and n-butyl; or R⁴ and R⁵ together with the bridging carbonatom form a radical selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,cyclopentenyl, cyclohexenyl, cycloheptenyl and cyclooctenyl; R⁶represents a hydrogen atom; a radical selected from the group consistingof methyl, ethyl, n-propyl, isopropyl, n-butyl and tert-butyl or aradical selected from the group consisting of cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl and cycloheptyl; R⁷ represents a hydrogen atomor a radical selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl and tert-butyl; R⁸ represents aradical selected from the group consisting of[1,2,3,4]-tetrahydronaphthyl, bicyclo[2.2.1]heptyl, cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl,cyclononyl, cyclodecyl, cycloundecyl and cyclododecyl, which may bebonded via a —(CH₂)—, —(CH₂)—(CH₂)— or —(CH₂)—(CH₂)—(CH₂)-group and/orsubsituted with 1, 2, 3 or 4 substituents selected from the groupconsisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl,tert-butyl, —OH, —O—CH₃ and —O—C₂H₅; or a radical selected from thegroup consisting of

which is in each case bonded to the pyrazoline compound of generalformula I in any position of the cyclic part of the aforementionedradicals including the NH-groups, preferably said radicals are bonded tothe pyrazoline compound of general formula I at the nitrogen atom of thecyclic part of the aforementioned radicals; and R¹¹ and R¹⁷,independently of one another, each represent a radical selected from thegroup consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl,isobutyl, sec-butyl, tert-butyl, n-pentyl, 2-pentyl, 3-pentyl andneo-pentyl; optionally in form of one of its stereoisomers, preferablyenantiomers or diastereomers, a racemate or in form of a mixture of atleast two of its stereoisomers, preferably enantiomers and/ordiastereomers, in any mixing ratio, or a corresponding N-oxide thereof,or a physiologically acceptable salt thereof, or a corresponding solvatethereof.
 17. A compound or salt according to claim 1 selected from thegroup consisting of [1]cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide hydro-chloride [2]trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide hydro-chloride [3]cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid azepan-1-ylamide [4]trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid azepan-1-ylamide [5]cis-[5-(4-Chloro-phenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-(4-cyclohexyl-piperazin-1-yl)-methanone[6]trans-[5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-(4-cyclohexyl-piperazin-1-yl)-methanone[7]cis-5-(4Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid pyrrolidin-1-ylamide [8]trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid pyrrolidin-1-ylamide [9]cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (4-methyl-piperidin-1-yl)-amide [10]trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (4-methyl-piperidin-1-yl)-amide [11]cis-[5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-piperidin-1-yl-methanone[12]trans-[5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-piperidin-1-yl-methanone[13]cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (hexahydro-cyclopenta[c]pyrrol-2-yl)-amide [14]trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (hexahydro-cyclopenta-[c]py-rrol-2-yl)-amide [15]cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (2,3-dihydro-indol-1-yl)-amide [16]trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (2,3-dihydro-indol-1-yl)-amide [17]cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid cyclobutylamide [18]5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid cyclohexyl methyl-amide [19]cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [20]trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [21]cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [22]trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [23]cis-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid methyl ester [24]trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid methyl ester [25]cis-5-(4Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid ethyl ester [26]trans-5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid ethyl ester [27]5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid cyclohe-xyl ester [28]5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4,4-dimethyl-4,5-dihydro-1-H-pyrazole-3-carboxylicacid [29]5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4,4-dimethyl-4,5-dihydro-1-H-pyrazole-3-carboxylicacid piperidin-1-ylamide [30]5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [31]5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylicacid [32]5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [33]5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-(2-hydroxy-ethyl)-4,5-di-hydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [34]5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-(2-hydroxy-ethyl)-4,5-di-hydro-1H-pyrazole-3-carboxylicacid [35]5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [36]5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [37]5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [38]5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [39]5-(4-chlorophenyl)-4-cyano-1-(2,4-dichlorophenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide[40]5-(4-Chloro-phenyl)-4-cyano-1-(2,4-dichloro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid [41]1-(2,4-Dichloro-phenyl)-5-(4-fluoro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [42]1-(2,4-Dichloro-phenyl)-4-ethyl-5-(4-fluoro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [43]1-(2,4-Dichloro-phenyl)-5-(4-fluoro-phenyl)-4,4-dimethyl-4,5-dihydro-1-H-pyrazole-3-carboxylicacid piperidin-1-ylamide [44] 1-(2,4-Dichloro-phenyl)-5-(4-fluorophenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylic acidpiperidin-1-ylamide [45]1-(2,4-Dichloro-phenyl)-5-(4-fluoro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [46]1-(2,4-Dichloro-phenyl)-5-(4-fluoro-phenyl)-4-(2-hydroxy-ethyl)-4,5-dihydro-1pyrazole-3-carboxylicacid piperidin-1-ylamide [47]1-(2,4-Dichloro-phenyl)-4-fluoromethyl-5-(4-fluoro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [48]1-(2,4-Dichlorophenyl)-5-(4-fluoro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [49]4-Cyano-1-(2,4-dichloro-phenyl)-5-(4-fluoro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [50]5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [51]5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [52]5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-yiamide [53]5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [54]5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [55]5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-(2-hydroxy-ethyl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [56]5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [57]5-(4-Bromo-phenyl)-1-(2,4-dichloro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [58]5-(4-Bromo-phenyl)-4-cyano-1-(2,4-dichloro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [59]cis-5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [60]trans-5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [61]cis-5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [62]trans-5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [63]5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [64]5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [65]5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [66]5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-(2-hydroxy-ethyl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [67]5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [68]5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [69]5-(5-Chloro-thiophen-2-yl)-4-cyano-1-(2,4-dichloro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [70]cis-5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [71]trans-5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [72]cis-5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [73]trans-5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [74]5-(5-Bromo-thiophen-2-yl)-1-(2,4-di-chloro-phenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [75]cis-5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [76]trans-5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [77]cis-5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [78]trans-5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [79]5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [80]5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [81]5-(5-Bromo-thiophen-2-yl)-1-(2,4-di-chloro-phenyl)-4-hydroxy-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [82]5-(5-Bromo-thiophen-2-yl)-1-(2,4-di-chloro-phenyl)-4-(2-hydroxy-ethyl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [83]5-(5-Bromo-thiophen-2-yl)-1-(2,4-di-chloro-phenyl)-4-fluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [84]5-(5-Bromo-thiophen-2-yl)-1-(2,4-di-chloro-phenyl)-4-formyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [85]5-(5-Bromo-thiophen-2-yl)-4-cyano-1-(2,4-dichloro-phenyl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide [86]cis-5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [87]trans-[5-(5-Chloro-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl]-piperidin-1-yl-methanone[88] cis-5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid [89]trans-5-(5-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [90]cis-5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [91]trans-5-(4-Bromo-thiophen-2-yl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid, 92(+)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 93(−)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 94cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide95trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide96cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid azepan-1-ylamide hydrochloride 97trans-5-(4-Chlorophenyl)-1-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid azepan-1-ylamide hydrochloride 98cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide99trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide100cis-5-(4-chlorophenyl)-N-(4-cyclopentylpiperazin-1-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 101cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-morpholino-4,5-dihydro-1H-pyrazole-3-carboxamide102cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(4-methylpiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide103cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(2,6-dimethylpiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide104cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (1,3-dioxo-1H,3H-benzo[de]isoquinolin-2-yl)-amide 105cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (1H,3H-benzo[de]isoquinolin-2-yl)-amide 106cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((R)-2-(methoxymethyl)pyrrolidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 107cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((S)-2-(methoxymethyl)pyrrolidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 108cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid (hexahydro-cyclopenta[c]pyrrol-2-yl)-amide hydrochloride 109cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide110trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide111cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide112trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide113cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(2-methylindolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide114cis-5-(4chlorophenyl)-N-(cyclohexylmethyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide115cis-5-(4-chlorophenyl)-N-(cycloheptylmethyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide116cis-5-(4-chlorophenyl)-N-cyclododecyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide117cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide118cis-N-(4-tert-butylcyclohexyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide119cis-5-(4-chlorophenyl)-N-cyclooctyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide120cis-N-(azocan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide121cis-N-(azocan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide122cis-azocan-1-yl(cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazol-3-yl)methanone123cis-5-(4-chlorophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide124cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-cycloheptyl-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide125trans-5-(4-chlorophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide126trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-cycloheptyl-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide127cis-5-(4-chlorophenyl)-N-(cyclohexylmethyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide128(+)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide129(−)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide130(−)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1R,2R)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide131(+)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-((1R,2R)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide132(+)-cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide133(−)-cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide134cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(4-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide135cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(4-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide136cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(3-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide137cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(3-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide138cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(2-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide139cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(2-hydroxypiperidin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide140cis-5-(4-chlorophenlyl)-1-(2,4dichlorophenyl)-4-methyl-N-(4-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide141cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(4-oxopiperidin-1yl)-4,5-dihydro-1H-pyrazole-3-carboxamide142cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(3-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide143cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(-3oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide144cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-N-(3,4-dihydropyridin-1(2H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide145cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(3,4-dihydropyridin-1(2H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide146cis-5-(4-chlorophenyl)-1-(2,4dichlorophenyl)-N-(5,6-dihydropyridin-1(2H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide147cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(5,6-dihydropyridin-1(2H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide148cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 149trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 150cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-py-razole-3-carboxylicacid cyclohexyl ester 151N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxamide1521-(2-chlorophenyl)-5-(4-chlorophenyl)-4,4-dimethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide153N-(azepan-1-yl)-1-(2-chlorophehyl)-5-(4-chlorophenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxamide154cis-5-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide 155trans-5-(4-Chloro-phenyl)-1-(2,4-dichlorophenyl)-4-trifluoromethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid piperidin-1-ylamide 156cis-N-(azepan-1-yl)-5-(4chlorophenyl)-1-(2,4-dichlorophenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide157trans-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide158cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide159 trans1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide1605-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-(piperidin-1-ylcarbamoyl)-4,5-dihydro-1H-pyrazole-4-carboxylicacid 1615-(4-chlorophenyl)-1-(2,4dichlorophenyl)-4,4-difluoro-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide162cis-5-(4-chlorophenyl)-4-cyano-1-(2,4-dichlorophenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide163cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-4-cyano-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide164cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-cyano-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide165cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-cyano-4,5-dihydro-1H-pyrazole-3-carboxamide166trans-5-(4-chlorophenyl)-4-cyano-1-(2,4-dichlorophenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide167trans-N-(azepan-1-yl)-5-(4-chlorophenyl)-4-cyano-1-(2,4-dichlorophenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide168trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-cyano-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide169cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-4,5-dihydro-1-pyrazole-3-carboxylicacid 170 trans-1-(2chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 171cis-5-(4chlorophenyl)-1-(2,4dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide172trans-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide173cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3carboxamide 174trans-1-(2-chlorophenyl)-5-(4-chlorophenyl-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide175cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide176trans-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide177cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide178trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide179cis-5-(4-chlorophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide180cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-N-cycloheptyl-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide181cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide182cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide183cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(indolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide184cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-ethyl-N-(indolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide185cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 186trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 187cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide188trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide189cis-5-(4-bromophenyl)-1-(2-chlorophenyl)4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide190trans-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide191cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide192cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide193cis-5-(4-bromophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide194cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-cycloheptyl-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxamide195cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide196cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide197cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(indolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide198cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-ethyl-N-(indolin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide199cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 200trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 201cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 202trans-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 203cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide204trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide205 cis5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide206trans-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide207cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2,4dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 208trans-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 209cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide210cis-N-(azepan-1-yl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide211cis-5-(4-bromophenyl)-N-cycloheptyl-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide212cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-cycloheptyl-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide213cis-5-(4-bromophenyl)-1-(2,4dichlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 214cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide215cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide216cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide217(+)-cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide218(−)-cis-5-(4bromophenyl)-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide219(+)-cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide220(−)-cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide221cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 222trans-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 223cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide224trans-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide225cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide226trans-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide227cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 228trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 229cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide230trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide231cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide232cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide233cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 234cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide235cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide236 cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-N-(indolin--yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide 237(+)-cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide238(−)-cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide239(+)-cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide240(−)-cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide241cis-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 242trans-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 243cis-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide244trans-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide245cis-1-(2-chlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide246trans-1-(2-chlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide247cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide248trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide249cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide250trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide251cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide252cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide253cis-1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide254cis-1-(2-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide255cis-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide256cis-1-(2-chlorophenyl)-N-(indolin-1-yl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide257(+)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide258(−)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide259(+)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide260(−)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-iodophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide261cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 262trans-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 263cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 264trans-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 265cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 266(+)-cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 267(−)-cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 268trans-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide269cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide270trans-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide271cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 272trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 273cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide274trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide275cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide276cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide277cis-1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 278cis-1-(2-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide279cis-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide280cis-1-(2-chlorophenyl)-N-(indolin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide281(+)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide282(−)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide283(+)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide284(−)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide285cis-1-(2,4-dichlorophenyl)-N-(4-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide286cis-1-(2-chlorophenyl)-N-(4-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide287cis-1-(2,4-dichlorophenyl)-N-(3-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide288cis-1-(2-chlorophenyl)-N-(3-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide289cis-1-(2,4-dichlorophenyl)-N-(2-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide290cis-1-(2-chlorophenyl)-N-(2-hydroxypiperidin-1-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide291cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(4-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide292cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(4-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide293cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(3-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide294cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(3-oxopiperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide295cis-1-(2,4-dichlorophenyl)-N-(3,4-dihydropyridin-1(2H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide296cis-1-(2-chlorophenyl)-N-(3,4-dihydropyridin-1(2H)-yl)-5-(4methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide297cis-1-(2,4-dichlorophenyl)-N-(5,6-dihydropyridin-1(2H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide298cis-1-(2-chlorophenyl)-N-(5,6-dihydropyridin-1(2H)-yl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide299cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide300trans-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide301cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide302trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide303cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide304trans-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin1-yl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxamide3051-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4,4-dimethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide306N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4,4-dimethyl-4,5-dihydro-1H-pyrazole-3-carboxamide3071-(2-chlorophenyl)-5-(4-methoxyphenyl)-4,4-dimethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3081-(2,4-dichlorophenyl)-4-formyl-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3091-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-3-(piperidin-1-ylcarbamoyl)-4,5-dihydro-1H-pyrazole-4-carboxylicacid 3101-(2,4-dichlorophenyl)-4-(2-hydroxyethyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3111-(2,4-dichlorophenyl)-4-(fluoromethyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide312cis-4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide313trans-4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide314cis-N-(azepan-1-yl)-4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide315trans-N-(azepan-1-yl)-4-cyano-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-3-carboxamide316cis-1-(2-chlorophenyl)-4-cyano-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide317trans-1-(2-chlorophenyl)-4-cyano-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3181-(2,4-dichlorophenyl)-4-hydroxy-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3191-(2-chloropheny!)-4,4-difluoro-5-(4methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3201-(2-chlorophenyl)-44formyl-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3211-(2-chlorophenyl)-5-(4-methoxyphenyl)-3-(piperidin-1-ylcarbamoyl)-4,5-dihydro-1H-pyrazole-4-carboxylicacid 3221-(2-chlorophenyl)-4-(2-hydroxyethyl)-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide3231-(2-chlorophenyl)-4-(flUoromethyl)-5-(4methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide324 1-(2-chlorophenyl)-4-hydroxy-5-(4-methoxyphenyl)-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide 325cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide326trans-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide327cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide328trans-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide329cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide330trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide331cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide332transN-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide333cis-N-cycloheptyl-1-(2,4dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide334cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-ethoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide335cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide336cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide337cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide338cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide339(+)-cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide340(−)-cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide341(+)-cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide342(−)-cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide343cis-1-(24dichlorophenyl-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide344trans-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide345cis-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide346trans-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide347cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4′methyl-4,5-dihydro-1H-pyrazole-3-carboxamide348trans-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide349cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide350trans-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide351cis-N-cycloheptyl-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide352cis-1-(2-chlorophenyl)-N-cycloheptyl-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide353cis-1-(2,4-dichlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 354cis-1-(2-chlorophenyl)-N-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide355cis-1-(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide356cis-1-(2-chlorophenyl)-5-(4-hydroxyphenyl)-N-(indolin-1-yl)-4-methyl4,5-dihydro-1H-pyrazole-3-carboxamide357(+)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide358(−)-cis-1-(2,4-dichlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide359(+)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide360(−)-cis-1-(2-chlorophenyl)-N-((1S,2S)-2-hydroxycyclohexyl)-5-(4-hydroxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide361cis-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 362trans-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 363 cis-1-(2 chlorophenyl)-5-(5-chlorothiophen2-yi)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid 364trans-1-(2-chlorophenyl)-5-(5-chlorothiophen-2-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 365cis-5-(5-bromothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 366trans-5-(5-bromothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-ethyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 367cis-1-(2,4-dichlorophenyl)-4-methyl-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid 368trans-1-(2,4-dichlorophenyl)-4-methyl-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxylicacid 369cis-1(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide370trans-1-(2,4dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide371cis-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide372trans-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide373cis-1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 374trans-1-(2,4dichlorophenyl)-4-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid 375cis-1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide376trans-1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide377cis-1-(2-chlorophenyl)-4-methyl-5-phenyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide378trans-1-(2-chlorophenyl)-4-methyl-5-phenyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide379cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamidehydrochloride 380trans-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide381cis-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide382trans-1-(2-chlorophenyl)-5-(4-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide383cis-N-(azepan-1-yl)-5-(4chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbothioamide384cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbothioamide385cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide386trans-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide387cis-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide388trans-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide389cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide390trans-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide391cis-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide392trans-1-(2-chlorophenyl)-5-(44luorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide393cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide394cis-N-(azepan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbothioamide395trans-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide396 cis-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide 397cis-N-(azepan-1-yl)-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carbothioamide398trans-1-(2-chlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide399cis-1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide400trans1-(2,4-dichlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide401cis-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide402trans-1-(2-chlorophenyl)-5-(4-ethoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide403cis-1(2,4-dichlorophenyl)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide404trans-1-(2,4dichoropheno)-5-(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide405 cis-1-(2-chlorophenyl)-5-(4hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide406trans-1-(2-chlorophenyl)-5(4-hydroxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carbothioamide407 7-(4-Chloro-phenyl)-6-(2,4-dichlorophenyl)-5,6diaza-spiro[2.4]hept-4-ene-4-carboxylic acid piperidin-1-ylamide 4086-(2,4-Dichloro-henyl)-7-(4-methoxy-phenyl)-5,6-diaza-spiro[2.4]hept-4-ene-4-carboxylicacid piperidin-1-ylamide409(+)-cis-N-N-((1S,2S)-2-(benzyloxy)cyclohexyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide[410]cis-1-(2,4-dichlorophehyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide[411]cis-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-IH-pyrazole-3-carboxamide [412](4R,5S)-1-(2,4dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [413]cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [414]cis-N-(azepan-1-yl)1-(2,4-dichlorophenyl)-5-(4fluorophenyl)-4methyl-4,5-dihydro-1H-pyrazole-3-carboxamide415cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-N-(indolin-1-yl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide416 trans-ethyl5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-(trifluoromethyl)-4,5-dihydro-1H-pyrazole-3-carboxylate417cis-1-(2,4-dichlorophenyl)-5-(4-fluorophenyl)-4ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 418cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 419(−)-cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide420(+)-cis-5-(4chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide421 trans-ethyl1-(2,4-dichlorophenyl)-4-methyl-5phenyl-4,5-dihydro-H-pyrazole-3-carboxylate422cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-((1R,2S,4R)-1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide423cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(3-methylcyclohexyl)-4,5-dihydro-1H-pyrazole-3-carboxamide424cis-5-(4-chlorophenyl)-1-(2,4dichlorophenyl)-4-methyl-N-(2-methylcyclohexyl)-4,5-dihydro-1H-pyrazole-3-carboxamide426trans-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 427cis-5-(5-chlorothiophen-2-yl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride 428cis-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride [429]1-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid [430]cis-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-3-carboxamidehydrochloride [431]trans-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide432cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide434cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamide436(+)-cis-N-((1S,2S)-2-(benzyloxy)cyclohexyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide437(−)-cis-N-((1R,2R)-2-(benzyloxy)cyclohexyl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide438cis-N-(azocan-1-yl)-1-(2,4-dichlorophenyl)-5-(4-methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide439cis-N-(azocan-1-yl)-1-(2-chlorophenyl)-5-(4methoxyphenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide440cis-N-(azocan-1-yl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide441cis-N-(azocan-1-yl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide442cis-N-(azocan-1-yl)-1-(2,4-dichlorophenyl)-5-(4fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide443cis-N-(azocan-1-yl)-1-(2-chlorophenyl)-5-(4-fluorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamide444(+)-cis-5(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid azepan-1-ylamide hydrochloride 445(−)-cis-(4-Chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxylicacid azepan-1-ylamide hydrochloride [446]cis-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamideN-oxide [447]cis-5-(4-chlorophenyl)-1-(2-chlorophenyl)-4-methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamideN-oxide [448]cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-l-(2,4-dichlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamideN-oxide [449]cis-N-(azepan-1-yl)-5-(4-chlorophenyl)-1-(2-chlorophenyl)-4-methyl-4,5-dihydro-1H-pyrazole-3-carboxamideN-oxide [450]cis-1-(2,4-dichlorophenyl)-5-(4methoxyphenyl)-4methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamideN-oxide and [451]cis-1-(2-chlorophenyl)-5-(4-rethoxyphenyl)-4methyl-N-(piperidin-1-yl)-4,5-dihydro-1H-pyrazole-3-carboxamideN-oxide; optionally in form of one of its stereoisomers, preferablyenantiomers or diastereomers, a racemate or in form of a mixture of atleast two of its stereoisomers, preferably enantiomers and/ordiastereomers, in any mixing ratio, or a corresponding N-oxide thereof,or a physiologically acceptable salt thereof, or a corresponding solvatethereof.
 18. Process for the preparation of a compound of generalformula I according to claim 1, wherein R⁵ represents hydrogen,characterized in that at least one compound of general formula II,

wherein R¹, X and R⁴ have the meaning according to claim 1, is reactedwith at least one compound of general formula III,

or a corresponding salt thereof, wherein R² has the meaning according toclaim 1, in a reaction medium, optionally in an inert atmosphere,optionally in the presence of at least one acid, to yield at least onecompound of general formula IV,

wherein R¹, X, R² and R⁴ have the meaning according to claim 1, which isoptionally isolated and/or purified, and at least one compound ofgeneral formula IV is reacted with an activating agent in a reactionmedium, optionally in an inert atmosphere, to yield at least onecompound of general formula V,

wherein R¹, X, R² and R⁴ have the meaning according to claim 1 and Arepresents a leaving group, which is optionally purified and/orisolated, and at least one compound of general formula V is reacted withat least one compound of general formula R³—H, wherein R³ has themeaning according to claim 1, in a reaction medium, optionally in aninert atmosphere, optionally in the presence of at least one baseselected from the group consisting of diisopropylethylamine,triethylamine, pyridine, dimethylaminopyridine and N-methylmorpholine,to yield at least one compound of general formula I, wherein R¹, R², X,R³ and R⁴ have the meaning according to claim 1 and R⁵ representshydrogen, which is optionally purified and/or isolated; or at least onecompound of general formula IV is reacted with at least one compound ofgeneral formula R³—H, wherein R³ represents a —NR⁷R⁸ moiety, whereby R⁷and R⁸ have the meaning according to claim 1, in a reaction medium, inthe presence of at least one coupling agent, optionally in the presenceof at least one base, to yield at least one compound of general formulaI, wherein R¹, R², X and R⁴ have the meaning according to claim 1, R³represents a —NR⁷R⁸ moiety and R⁵ represents hydrogen, which isoptionally purified and/or isolated.
 19. Process for the preparation ofa compound of general formula I according to claim 1, wherein R⁵represents hydrogen, characterized in that at least one compound ofgeneral formula R¹—C(═O)—H (general formula VIl), wherein R¹ has themeaning according to claim 1, is reacted with at least one compound ofgeneral formula VI,

wherein R⁴ and X have the meaning according to claim 1 and R′ representsa linear or branched C₁₋₆-alkyl radical, a potassium cation or a sodiumcation, in a reaction medium, optionally in an inert atmosphere,optionally in the presence of at least one base, to yield at least onecompound of general formula II,

wherein R¹, X and R⁴ have the meaning according to claim 1, which isoptionally purified and/or isolated, and at least one compound ofgeneral formula II is reacted with an activating agent in a reactionmedium, optionally in an inert atmosphere, to yield at least onecompound of general formula VIII,

wherein R¹, X and R⁴ have the meaning according to claim 1 and Arepresents a leaving group, which is optionally purified and/orisolated, and at least one compound of general formula VII is reactedwith at least one compound of general formula R³—H, wherein R³ has themeaning according to claim 1, in a reaction medium, optionally in aninert atmosphere, optionally in the presence of at least one baseselected from the group consisting of diisopropylethylamine,triethylamine, pyridine, dimethylaminopyridine and N-methylmorpholine,to yield at least one compound of general formula IX,

wherein R¹, X, R³ and R⁴ have the meaning according to claim 1, which isoptionally purified and/or isolated; or at least one compound of generalformula II is reacted with at least one compound of general formulaR³—H, wherein R³ represents a —NR⁷R⁸ moiety, whereby R⁷ and R⁸ have themeaning according to claim 1, in a reaction medium, in the presence ofat least one coupling agent, optionally in the presence of at least onebase, to yield at least one compound general formula IX, wherein R³represents a —NR⁷R⁸ moiety, which is optionally purified and/orisolated, and at least one compound of general formula IX is reactedwith at least one compound of general formula III,

wherein R² has the meaning according to claim 1, in a reaction medium,optionally in an inert atmosphere, optionally in the presence of atleast one acid, to yield at least one compound of general formula I,wherein R¹, X, R², R³ and R⁴ have the meaning according to claim 1 andR⁵ represents hydrogen, which is optionally purified and/or isolated.20. Process for the preparation of a compound of general formula Iaccording to claim 1, wherein R⁵ is unlike hydrogen, characterized inthat at least one compound of general formula R¹—C(═O)—H (generalformula VII), wherein R¹ has the meaning according to claim 1, isreacted with at least one compound of general formula VIb,

wherein R⁴, R⁵ and X have the meaning according to claim 1, R⁵ is unlikehydrogen and R′ represents a linear or branched C₁₋₆-alkyl radical, apotassium cation or a sodium cation, in a reaction medium, optionally inan inert atmosphere, optionally in the presence of at least one base, toyield at least one compound of general formula XXXI,

wherein R¹, R⁴, R⁵ and X have the meaning according to claim 1, R⁵ isunlike hydrogen, and R′ represents a linear or branched C₁₋₆-alkylradical, a potassium cation or a sodium cation, and at least onecompound of general formula XXXXI is reacted with a reagent, thattransforms a hydroxyl group into a leaving group, preferably with areagent selected from the group consisting of methansulfonylchloride andtoluolsulfonylchloride, in a reaction medium, optionally in the presenceof at least one base, preferably in the presence of at least one baseselected from the group consisting of triethylamine,diisopropylethylamine, pyridine and N-methylmorpholine, to yield acompound of general formula XXXXII,

wherein R¹, R⁴, R⁵ and X have the meaning according to claim 1, R⁵ isunlike hydrogen, R′ represents a linear or branched C₁₋₆-alkyl radical,a potassium cation or a sodium cation, and LG is a leaving group,preferably mesyl or tosyl; and at least one compound of general formulaXXXXII is reacted with at least one compound of general formula III,

or a corresponding salt thereof, wherein R² has the meaning according toclaim 1, in a reaction medium, optionally in an inert atmosphere,optionally in the presence of at least one acid, to yield at least onecompound of general formula lVb,

wherein R¹, X, R², R⁴ and R⁵ have the meaning according to claim 1 andR⁵ is unlike hydrogen, which is optionally isolated and/or purified, andat least one compound of general formula lVb is reacted with anactivating agent in a reaction medium, optionally in an inertatmosphere, to yield at least one compound of general formula Vb,

wherein R¹, X, R², R⁴ and R⁵ have the meaning according to claim 1, R⁵is unlike hydrogen and A represents a leaving group, which is optionallypurified and/or isolated, and at least one compound of general formulaVb is reacted with at least one compound of general formula R³—H,wherein R³ has the meaning according to claim 1, in a reaction medium,optionally in an inert atmosphere, optionally in the presence of atleast one base selected from the group consisting ofdiisopropylethylamine, triethylamine, pyridine, dimethylaminopyridineand N-methylmorpholine, to yield at least one compound of generalformula I, wherein R¹, R², X, R³, R⁴ and R⁵ have the meaning accordingto claim 1 and R⁵ is unlike hydrogen, which is optionally purifiedand/or isolated; or at least one compound of general formula lVb isreacted with at least one compound of general formula R³—H, wherein R³represents a —NR⁷R⁸ moiety, whereby R⁷ and R⁸ have the meaning accordingto claim 1, in a reaction medium, in the presence of at least onecoupling agent, optionally in the presence of at least one base, toyield at least one compound of general formula I, wherein R¹, R², X, R⁴and R⁵ have the meaning according to claim 1, R³ represents a —NR⁷R⁸moiety and R⁵is unlike hydrogen, which is optionally purified and/orisolated.
 21. Medicament comprising at least one compound according toclaim 1 including the aformenentioned excluded compounds and optionallyat least one physiologically acceptable auxiliary agent.
 22. Medicamentaccording to claim 21 for the modulation of cannabinoid-receptors,preferably cannabinoid 1 (CB₁) receptors, for the prophylaxis and/ortreatment of disorders of the central nervous system, disorders of theimmune system, disorders of the cardiovascular system, disorders of theendocrinous system, disorders of the respiratory system, disorders ofthe gastrointestinal tract or reproductive disorders.
 23. Medicamentaccording to claim 21 for the prophylaxis and/or treatment of foodintake disorders, preferably bulimia, anorexia, cachexia, obesity, typeII diabetes mellitus (non-insuline dependent diabetes mellitus), morepreferably obesity.
 24. Medicament according to claim 21 for theprophylaxis and/or treatment of psychosis.
 25. Medicament according toclaim 21 for the prophylaxis and/or treatment of alcohol abuse and/oralcohol addiction, nicotine abuse and/or nicotine addiction, drug abuseand/or drug addiction and/or medicament abuse and/or medicamentaddiction, preferably drug abuse and/or drug addiction and/or nicotineabuse and/or nicotine addiction.
 26. Medicament according to claim 21for the prophylaxis and/or treatment of cancer, preferably for theprophylaxis and/or treatment of one or more types of cancer selectedfrom the group consisting of brain cancer, bone cancer, lip cancer,mouth cancer, esophageal cancer, stomach cancer, liver cancer, bladdercancer, pancreas cancer, ovary cancer, cervical cancer, lung cancer,breast cancer, skin cancer, colon cancer, bowel cancer and prostatecancer, more preferably for the prophylaxis and/or treatment of one ormore types of cancer selected from the group consisting of colon cancer,bowel cancer and prostate cancer.
 27. Medicament according to claim 21for the prophylaxis and/or treatment of one or more disorders selectedfrom the group consisting of bone disorders, preferably osteoporosis(e.g. osteoporosis associated with a genetic predisposition, sex hormonedeficiency, or aging), cancer-associated bone disease or Paget's diseaseof bone; schizophrenia, anxiety, depression, epilepsy, neurodegenerativedisorders, cerebella disorders, spinocerebella disorders, cognitivedisorders, cranial trauma, head trauma, stroke, panic attacks,peripheral neuropathy, glaucoma, migraine, Morbus Parkinson, MorbusHuntington, Morbus Alzheimer, Raynaud's disease, tremblement disorders,compulsive disorders, senile dementia, thymus disorders, tardivedyskinesia, bipolar disorders, medicament-induced movement disorders,dystonia, endotoxemic shock, hemorrhagic shock, hypotension, insomnia,immunologic disorders, sclerotic plaques, vomiting, diarrhea, asthma,memory disorders, pruritus, pain, or for potentiation of the analgesiceffect of narcotic and non-narcotic analgesics, or for influencingintestinal transit.
 28. Use of at least one substituted pyrazolinecompound according to claim 1 for the preparation of a medicament forthe modulation of cannabinoid-receptors, preferably cannabinoid 1 (CB₁)receptors, for the prophylaxis and/or treatment of disorders of thecentral nervous system, disorders of the immune system, disorders of thecardiovascular system, disorders of the endocrinous system, disorders ofthe respiratory system, disorders of the gastrointestinal tract orreproductive disorders.
 29. Use of at least one substituted pyrazolinecompound according to claim 1 for the preparation of a medicament forthe prophylaxis and/or treatment of food intake disorders, preferablybulimia, anorexia, cachexia, obesity, type II diabetes mellitus(non-insuline dependent diabetes mellitus), more preferably obesity. 30.Use of at least one substituted pyrazoline compound according to claim 1for the preparation of a medicament for the prophylaxis and/or treatmentof psychosis.
 31. Use of at least one substituted pyrazoline compoundaccording to claim 1 for the preparation of a medicament for theprophylaxis and/or treatment of alcohol abuse and/or alcohol addiction,nicotine abuse and/or nicotine addiction, drug abuse and/or drugaddiction and/or medicament abuse and/or medicament addiction,preferably drug abuse and/or drug addiction and/or nicotine abuse and/ornicotine addiction.
 32. Use of at least one substituted pyrazolinecompound according to claim 1 for the preparation of a medicament forthe prophylaxis and/or treatment of cancer, preferably for theprophylaxis and/or treatment of one or more types of cancer selectedfrom the group consisting of brain cancer, bone cancer, lip cancer,mouth cancer, esophageal cancer, stomach cancer, liver cancer, bladdercancer, pancreas cancer, ovary cancer, cervical cancer, lung cancer,breast cancer, skin cancer, colon cancer, bowel cancer and prostatecancer, more preferably for the prophylaxis and/or treatment of one ormore types of cancer selected from the group consisting of colon cancer,bowel cancer and prostate cancer.
 33. Use of at least one substitutedpyrazoline compound according to claim 1 for the preparation of amedicament for the prophylaxis and/or treatment of one or more disordersselected from the group consisting of bone disorders, preferablyosteoporosis (e.g. osteoporosis associated with a geneticpredisposition, sex hormone deficiency, or aging), cancer-associatedbone disease or Paget's disease of bone; schizophrenia, anxiety,depression, epilepsy, neurodegenerative disorders, cerebella disorders,spinocerebella disorders, cognitive disorders, cranial trauma, headtrauma, stroke, panic attacks, peripheral neuropathy, glaucoma,migraine, Morbus Parkinson, Morbus Huntington, Morbus Alzheimier,Raynaud's disease, tremblement disorders, compulsive disorders, seniledementia, thymic disorders, tardive dyskinesia, bipolar disorders,medicament-induced movement disorders, dystonia, endotoxemic shock,hemorrhagic shock, hypotension, insomnia, immunologic disorders,sclerotic plaques, vomiting, diarrhea, asthma, memory disorders,pruritus, pain, or for potentiation of the analgesic effect of narcoticand non-narcotic analgesics, or for influencing intestinal transit. 34.A method of modulating cannabinoid-receptors, preferably cannabinoid 1(CB₁) receptors, of preventing and/or treating disorders of the centralnervous system, disorders of the immune system, disorders of thecardiovascular system, disorders of the endocrinous system, disorders ofthe respiratory system, disorders of the gastrointestinal tract orreproductive disorders, comprising administering to a subject,preferably a human, therapeutically effective amount of at least onesubstituted pyrazoline compound according to claim
 1. 35. A method oftreating food intake disorders, preferably bulimia, anorexia, cachexia,obesity, type II diabetus mellitus (non-insuline dependent diabetesmellitus), more preferably obesity, comprising administering to asubject, preferably a human, a therapeutically effective amount of atleast one substituted pyrazoline compound according to claim
 1. 36. Amethod of treating psychosis comprising administering to a subject,preferably a human, a therapeutically effective amount of at least onesubstituted pyrazoline compound according to claim
 1. 37. A method oftreating alcohol abuse and/or alcohol addiction, nicotine abuse and/ornicotine addiction, drug abuse and/or drug addiction and/or medicamentabuse and/or medicament addiction, preferably drug abuse and/or drugaddiction and/or nicotine abuse and/or nicotine addiction, comprisingadministering to a subject, preferably a human, a therapeuticallyeffective amount of at least one substituted pyrazoline compoundaccording to claim
 1. 38. A method of treating of cancer, preferably forthe prophylaxis and/or treatment of one or more types of cancer selectedfrom the group consisting of brain cancer, bone cancer, lip cancer,mouth cancer, esophageal cancer, stomach cancer, liver cancer, bladdercancer, pancreas cancer, ovary cancer, cervical cancer, lung cancer,breast cancer, skin cancer, colon cancer, bowel cancer and prostatecancer, more preferably for the prophylaxis and/or treatment of one ormore types of cancer selected from the group consisting of colon cancer,bowel cancer and prostate cancer comprising administering to a subject,preferably a human, a therapeutically effective amount of at least onesubstituted pyrazoline compound according to claim
 1. 39. A method oftreating one or more disorders selected from the group consisting ofbone disorders, preferably osteoporosis (e.g. osteoporosis associatedwith a genetic predisposition, sex hormone deficiency, or ageing),cancer-associated bone disease or Paget's disease of bone;schizophrenia, anxiety, depression, epilepsy, neurodegenerativedisorders, cerebellar disorders, spinocerebellar disorders, cognitivedisorders, cranial trauma, head trauma, stroke, panic attacks,peripheric neuropathy, glaucoma, migraine, Morbus Parkinson, MorbusHuntington, Morbus Alzheimer, Raynaud's disease, tremblement disorders,compulsive disorders, senile dementia, thymic disorders, tardivedyskinesia, bipolar disorders, medicarnent-induced movement disorders,dystonia, endotoxemic shock, hemorrhagic shock, hypotension, insomnia,immunologic disorders, sclerotic plaques, vomiting, diarrhoea, asthma,memory disorders, pruritus, pain, or for potentiation of the analgesiceffect of narcotic and non-narcotic analgesics, or for influencingintestinal transit, comprising administering to a subject, preferably ahuman, a therapeutically effective amount of at least one substitutedpyrazoline compound according to claim 1.